Dr. Basavaraj K. Nanjwade M.Pharm., Ph.D. Professor of Pharmaceutics Department of Pharmaceutics, KLE University College of Pharmacy, Belgaum - 590010, Karnataka, INDIA Cell No: 00919742431000 Phone No: 00918312471399 Fax No: 00918312472387
Abstract: Purpose: The aim was to develop and evaluate curcumin ethosomes for transdermal delivery. Methods: Curcumin
ethosomes was prepared by cold method. The prepared ethosomes were characterized for their entrapment
efficiency, particle size, zeta potential, SEM, degree of deformability, FTIR, DSC, and XRD studies. In
final phase of formulation development, ethosomal formulations ET-1 to ET-5 were converted to gels G-1 to
G-5 respectively using 2% w/w of carbopol 940. The in vitro drug permeation study of ethosomal gels (G-1 to
G-5) were compared with gel (G-6) containing free curcumin drug. Formulation G-6 also made using 2% w/w
of carbopol 940. The in vivo bioavailability study of best formulation G-5 was compared with G-6. Stability study
of best formulation G-5 was performed at 5 C±3 C and 25 C±2 C for 30 days. The best formulation was
selected based on in vitro drug permeation study. Results: The in vitro drug permeation of G-1 to G-5 (ethosomal
gel) was higher than G-6 (gel containing free curcumin). The in vivo bioavailability of best formulation G-5
was higher than G-6. Formulation G-5 was more stable at 5 C ± 3 C for 30 days. Conclusions: Bioavailability
and therapeutic value of curcumin is increased by ethosomal gel.
Abstract: The present study aims to prepare nanoparticles in form of aquasomes with Etoposide as a low solubility drug mode.
Etoposide aquasomes were obtained through the formation of an inorganic core of calcium phosphate covered with a
Lactose film and further adsorption of the Etoposide. The formulations were then characterized with respect to size and
its surface morphology, zeta potential, entrapment efficiency, in vitro drug release profile, stability studies, in vivo tissue
distribution studies and in vivo pharmacokinetic studies. The formulated Etoposide nanoparticles were spherical with a
diameter ranging from 150 to 250 nm. Highest entrapment efficiency was found to be 88.41%. Highest cumulative percent
drug release was observed with F-5 (79.19%) in 120 hrs. Formulation F-5 with optimal particle size, high entrapment
efficiency and satisfactory in vitro release was selected for in vivo studies. The average targeting efficiency of drug loaded
nanoparticles was found to be 42.54% of the injected dose in liver, 12.22% in lungs, 4.14% in kidney and 25.12% in
spleen. The results revealed that, the drug loaded nanoparticles showed preferential drug targeting to liver followed by
spleen, lungs and kidney. The in-vivo studies were carried out by HPLC method to assess the pharmacokinetic parameters
like Cmax tmax, AUC, t1/2. Formulation F-5 was selected for this study and it showed Cmax value of 1.48 g/ml, tmax of
2 hrs, AUC was 20.40 g/ml and a t1/2 of 13.5 hrs. Stability studies indicated that 4C is the most suitable temperature
for storage of Etoposide nanoparticles. This drug delivery is endowed with several exclusive advantages and hence holds
potential for further research and clinical application.
Abstract: The present study aimed to conceptualize pulsatile principles to develop a time dependent programmable pulsincap drug
delivery system of 5-Fluorouracil, intended for chronotherapy in colorectal cancer. Microcapsules of 5-Fluorouracil were
formulated by emulsification-solvent evaporation method using three different drug (5-Fluorouracil): polymer (Eudragit
L-100 55) ratio (viz., 1:1, 1:2, & 1:3) and their physico-chemical properties were evaluated. The optimized formulation
MC-2 was filled into formaldehyde treated hard gelatin capsules using different quantities (20 mg & 30 mg) of Gellan
gum, Guar gum, Xanthan gum and Locust bean gum as hydrogel plugs to maintain a suitable lag period. Further modified
capsules were coated with Eudragit S-100 (15%). In-vitro release studies of all the formulations showed that there was no
drug release in acidic pH (0.1 N HCl) and in simulated intestinal fluid (pH 6.8 phosphate buffer). Drug release occurred
in pH 7.4 upto 24 hrs in a controlled manner depending upon the quantity of hydrogel plug. All the formulations followed
first order drug release kinetics and showed anomalous transport i.e., a combined mechanism of pure diffusion and
Case II transport. Gamma scintigraphic studies concluded that the system released the drug in lower parts of GIT after
a programmed lag time. In-vivo studies revealed that pulsincap system of formulation (F-3) showed good bioavailability
compared to oral solution. Accelerated stability studies indicated that formulation F-3 was quite stable.
Abstract: In the present work an attempt has been made to prepare FDT of Lomefloxacin HCl with an view to enchance the patient compliance, and provide a quick onset of action, increasing the solubility and masking its bitter taste. Taste masking and solubility was enchanced by complexing Lomefloxacin HCl with hydroxyl propyl β-cyclodextrin (HP-βCD) by solvent evaporation method. Prepared complex was further compressed into tablets by direct compression using different superdisintegrant like Sodium starch glycolate, Croscarmellose sodium, Polyplasdone XL-10 in different concentration such as 1%, 1.5%, 2 % using aspartame as a sweetner and aerosil as lubricant. The drug release from FDT increase with increasing the concentration of superdisintegrants and was found to be highest with formulation F6 containing 1.5 % Croscarmellose Sodium and was consider to be the best formulation which release upto 100.68 % in 45 min. In vivo studies revealed that FDT of formulation (F 6) showed good bioavailability compared to conventional tablet. The fast dissolving tablet with HP-βCD complex can be formulated using different superdisintegrants by Direct Compression technique and was found to be disintegrate less than 2 minute, which provide faster effect and better patient compliance.
Abstract: Nanostructured lipid carriers (NLC) developed from mixtures of solid lipid and spatially incompatible liquid lipid by solvent
diffusion method. This new type of lipid nanoparticles offers the advantage of improved drug loading capacity and release
properties. In this study, Glyceryl distearate and Glyceryl behenate were chosen as solid lipid and Glyceryl triacetate
used as liquid lipid. Ubidecarenone used as model drug was incorporated into the NLC. The influences of different type
of solid lipid and liquid lipid concentration on physiochemical properties of the NLC were characterized. As a result, the
drug encapsulation efficiencies were improved by adding the liquid lipid into the solid lipid of nanoparticles. NLC had
higher encapsulation efficiency and drug release. In addition, in vivo study showed that the antioxidant activity of the
Ubidecarenone (Co. Q10 NLC) was more effective than the Ubidecarenone (Coenzyme Q10) solution form on DPPH
scavenging, anti-lipid peroxidation, lowers the effect of amnesia induced by scopolamine and increased bioavailability
observed in Cmax, Tmax, and AUC. These results indicated that nanostructured lipid formulation of Ubiquinone (Coenzyme
Q10) has more antioxidant activity than that of solution form and it can be used to reduce the oxidative stress and to
increase the antioxidant enzyme activity in many neurodegenerative disorders such as Alzheimer’s disease, Parkinson’s
disease etc.
Abstract: In the present work an attempt has been made to prepare binary solid
complex, Prulifloxacin and Lomefloxacin HCl with soluplus to enchance
physicochemical properties like solubility. Solubility was enhanced by
complexing Prulifloxacin and Lomefloxacin HCl with novel soluplus by
fusion (Co-melt) method. Prepared complex was further characterized by
FT-IR, DSC. Solid state characterization of the pure drug and its mixture
with various excipients were studied. The soluplus is novel amphiphillic
graft polymer which tunes the physicochemical properties of the poorly
water soluble drugs.
Abstract: The present study deals with the formulation and
in-vitro characterization of tamoxifen loaded
stealth liposomes. Passive targeting by stealth
liposomes, once combined with efficient
intracellular delivery, may be a very useful strategy
to improve the antitumor efficacy for the
anticancer agents. Stealth liposomes were
prepared by using Cholesterol, DMPC, DSPC, and
Polyethylene Glycol 4000 (PEG 4000) in order to
achieve prolonged circulation time and sustained
release. The prepared liposomes were evaluated
for size, shape, profile, degree of drug entrapment,
and in-vitro release efficiency. The effect of
various formulation and drug release was
investigated.
Abstract: To enhance the bioavailability of the poorly
water-soluble drug Aceclofenac, a lipidnanoemulsion
comprising ethanolic solution of
phospholipid 90 G and tween 80 in 1:1 ratio
(Smix), triacetin and anseed oil as oil phase and
distilled water as aqueous phase, in the ratio of
55:15:30 (% w/w) was developed by
constructing pseudo-ternary phase diagrams
and evaluated for viscosity, % transmittance,
and surface morphology of nanoemulsions. In
vitro diffusion (release) of Aceclofenac from
three different bases to an aqueous receptor
phase through cellophane membrane was
monitored spectrophotometrically at 273 nm.
Compared with hydroalcoholic drug solution,
oily solution, and conventional emulsion and
suspension. The lipid-nanoemulsion showed
increase in drug release compared to drug
suspension. This may be attributed to increased
solubility of the drug from nanosized emulsion.
Abstract: This study was carried out to evaluate and compare the tissue distribution profile of
tamoxifen citrate, when administered intravenously (i.v.) as a simple solution or when
encapsulated into stealth liposomes with an average diameter of 479 nm. Passive targeting by
stealth liposomes, once combined with efficient intracellular delivery, may be a very useful
strategy to improve the antitumor efficacy of the anticancer agents. Natural ability of liposomes
to target cancer cells (tumor) due to enhanced permeability and retention (EPR) effect and
polyethylene glycol (PEG) coating of stealth liposomes which is inert in the body, allows for
longer circulatory life for the drug delivery mechanism results in enhanced accumulation of
tamoxifen in tumor. Tamoxifen loaded stealth liposomes (TSL) were prepared with thin film
hydration method by using cholesterol, DMPC, DSPC, and polyethylene glycol-4000 (PEG-
4000) in order to achieve prolonged circulation time and sustained release. In vivo tissue
distribution study was carried out in Sprague-Dawley rats having mammary tumor induced by
chemical carcinogenDMBA (7,12-Dimethylbenz(a)anthracene). After intravenous administration,
the primary site of accumulation for the TSL was tumor accounting up to 36% after 6 h post
injection compared to 6% observed with non-formulated tamoxifen. The results indicate that,
TSL may present a promising delivery system to achieve preferential tumor-targeting.
Abstract: Introduction: Solid dispersions are one of the most promising strategies to improve the oral bioavailability of sparingly water soluble drugs. Drug
particle size reduction improved the drug wettability and bioavailability significantly. Candesartan cilexetil (CAN), a sparingly water-soluble drug offers
challenges in developing a drug product with adequate bioavailability. Materials and methods: Polyvinylpyrrolidone K30 incorporated in solid
dispersions (PVP K30) in different drug-to-carrier ratios to increase its saturation solubility and dissolution rate for improving bioavailability. This
further reduces variability in systemic exposure. The kneading technique prepared the CAN dispersions. Differential Scanning Calorimetry (DSC),
Fourier Transformation-Infrared spectroscopy (FTIR) and Powder X-ray Diffraction (PXDR) characterized dispersions in solid-state. Key findings:
The results from DSC, FTIR and PXDR analyses of solid dispersions suggested that CAN might exist as an amorphous state and entrapped in polymer
matrix. Increasing polymer concentration increased the solubility of the drug. The solid dispersion was stable under accelerated storage conditions.
Conclusion: This study showed the rate of dissolution and magnitude of the apparent solubility were found to be significantly higher for amorphous
CAN than for crystalline CAN at 1: 2 drug to polymer ratio. In conclusion, PVPK30 enhanced dissolution of CAN as a hydrophilic carrier which provides
a promising way to improve the solubility and dissolution rate of CAN.
Abstract: The field of ocular drug delivery is one of the interesting and challenging endeavors facing the pharmaceutical scientist. Novel approaches for ophthalmic drug delivery need to be established to increase the ocular bioavailability by overcoming the inherent drawbacks of conventional dosage forms. In situ hydrogels are instilled as drops into the eye and undergoes a sol-to-gel transition in the cul-de-sac, improved ocular bioavailability by increasing the duration of contact with corneal tissue, thereby reducing the frequency of administration. The purpose of the present work was to develop an ophthalmic drug delivery system using three different gelling agents with different mechanisms for in situ gelation of Moxifloxacin hydrochloride, a fluoroquinolone antibiotic. polyox (a pH-sensitive gelling agent), sodium alginate (an ion-sensitive gelling agent), and poloxamer (a temperature-sensitive gelling agent) were employed for the formation of in situ hydrogel along with HPMC K4M as viscofying agent, which increases the residence time of the drug in the ocular cavity. The promising formulations MF4, MF5, and MF9 were evaluated for pH, drug content, in vitro gelation, in vitro drug release, in vivo drug release, ocular irritation, and stability. Percent drug content of 98.2, 98.76, and 99.43%; viscosity of 15.724 × 100, 16.108 × 100, and 15.213 × 100 cP at 20 rpm, cumulative percent release of 75.364, 74.081, and 71.752%, and C max of 1,164.16, 1,187.09, and 1,220.58 ng/ml was observed for formulation MF4, MF5, and MF9, respectively. The developed formulations were therapeutically efficacious, stable, and non-irritant and provided sustained release of the drug over 8 h.
Abstract: Paclitaxel (PTX) is an antineoplastic agent, commonly used to treat some leukemias, Hodgkin’s
lymphoma, as well as cancers of the bladder, breast, stomach, lung, ovaries, thyroid, soft tissue
sarcoma, multiple myeloma, and others. However, expansion of the clinical utility of Paclitaxel has
been limited by its liver and cardiac toxicity and myelosuppression. In the present study proliposome
drug delivery system for Paclitaxel was developed, which will increase the efficacy and reduce the
toxicity. Proliposomal drug delivery system for Paclitaxel was prepared by modified film hydration
method using different ratio of two different carriers and same coating polymer with different concentrations.
Formulations F1, F2 and F3, F4 were prepared by using Egg phosphatidylglycerol (EPG)
and Distearoyl phosphatidylcholine (DSPC) as a carrier respectively and coating polymer PEGylated
phospholipid (MPEG 2000-DSPE, Sodium salt). All the formulations were compared in terms
of particle size, zeta potential, encapsulation efficiency, in vitro drug release. Optimized formulation
F2 was evaluated for pharmacokinetics parameters and stability studies as per ICH guidelines. Stability
studies revealed that 4 C is the most suitable temperature for storage of proliposomal drug
delivery system for Paclitaxel.
Abstract: The purpose of this research was to develop a novel gastroretentive drug delivery system based on effervescent technology for controlled
delivery of active agent. Glipizide, a poorly soluble drug has been used as a model drug and an attempt has been made to improve the solubility
of drug by the incorporation of accelerating agents, such as dispersant, alkalizing agent in conjunction with hydrophilic swellable polymer such
as hydroxypropylmethylcellulose and present it in the form of gastroretentive floating tablets, which are designed to provide the desired controlled
and complete release of drug for a prolonged period of time. Floating tablets were prepared by direct compression method. Hydroxypropylmethylcellulose
(HPMC K15M, HPMC K100M) and Carbopol 940P were incorporated for gelforming properties. Buoyancy was achieved by adding
an effervescent mixture of sodium bicarbonate and anhydrous citric acid. The optimized formulation (F7) exhibited 98.60 % drug release in 24 h,
while the buoyancy lag time was 140 s. In vitro drug release kinetics were found to follow both the zero order and the Korsmeyer and Peppas
equation. The release of glipizide from the formulations was found to be non-Fickian type. Evaluation of gastric retention using X-ray imaging
studies were performed on rabbit to justify the increased gastric residence time of the dosage form in the stomach, based on the floating principle.
Optimized formulation (F7) showed no significant change in physical appearance, drug content, total buoyancy time, or in vitro dissolution pattern
after storage at 40 °C/75 % relative humidity for 1 month.
Abstract: The objectives of this study were to prepare and characterize the
novel Lomefloxacin-Salicylic acid and Lomefloxacin-Urea to
demonstrate the enhanced dissolution of Lomefloxacin by co crystal
formation in comparison with the pure drug. Lomefloxacin-Salicylic
acid and Lomefloxacin-Urea co crystal was prepared using greener
technique cogriding with aim of enhancing their dissolution rate
sand their bioavailability. DSC, IR and PXRD were used to
characterize the novel solid form. The dissolution and chemical
stability were assessed and compared with marketed Maxaquin.
Pharmaceutical co crystals are new solid forms with
physicochemical properties that appear promising for drug product
development. Novel solid co crystals with distinct melting. DSC,
FTIR and PXRD data was obtained. The co crystal of lomefloxacin
with salicylic acid (SA) has been shown to have higher solubility
than lomefloxacin. In this study, we aimed to characterize the pure
drug and the co crystals with the salicylic acid and urea.
Remarkably, two new co crystals of lomefloxacin were discovered in
this study. The study indicates that the improved aqueous solubility
of the co crystals leads to improved dissolution of Lomefloxacin.
Thus, the co crystals are a viable alternative solid form that can
improve the dissolution rate and bioavailability of poorly soluble
drugs. Subsequently, differential scanning calorimetry was used to
investigate the co crystal formation. The formation of co crystals
was also verified using liquid-assisted grinding. The spectral
patterns of lomefloxacin, salicylic acid and the complex were
different. The physicochemical properties such as solubility and
dissolution rate of this complex will be further investigated.
Abstract: Novel solid forms of prulifloxacin with various GRAS coformers are discussed with its in vivo
antimicrobial activity. To evaluate the in vitro antimicrobial activity of prulifloxacin and its
novel solid forms on the isolates of bacteria. Poor aqueous solubility is a major barrier in the
development of new chemical entities as well as older drug molecules as pharmaceutical
formulations. Over 80% of marketed drugs are sold as tablets; 40% drugs in the market have
poor solubility and, more alarmingly, almost 80−90% of drug molecules that are at advanced
stages of drug development will pose a solubility problem. The minimum inhibitory
concentration (MIC) and antitubercular activity of prulifloxacin and its novel solid forms were
measured using method of Clinical Laboratory Standards Institute (CLSI). Prulifloxacin and
its novel solid forms were found to have antimicrobial activity against various isolates. The
MIC was found to be high in all novel solid forms against pure prulifloxacin studied. The MIC
was found to be less than 0.2 μg/ml for all the title compounds against Staphylococcus aureus
and the range 1.6 - 0.2 μg/ml against Escherichia coli. Prulifloxacin is a fluoroquinolone
antibiotic that has been approved in several European countries for the treatment of lower
urinary tract infections and exacerbations of chronic bronchitis. In summary, prulifloxacin and
its novel solid forms appears to be a promising agent for the treatment of bacterial isolates. Its
antifungal and antitumor activity study are in progress.
Abstract: A novel series of Substituted diaryl Imidazole [2, 1, b] benzothiazole derivatives (8a-y) were synthesized by condensation reaction between 2-amino benzothiazole derivatives (3a-g) and substituted α-bromo-1, 2-(substituted) diaryl-1-ethanones (7a-i). The structures of the synthesized compounds were established by IR, 1H NMR, 13C NMR and Mass spectroscopical data. The compounds (8a-y) were evaluated for their in-vitro cytotoxic activity on murine (B16F10) and human (MCF-7) cancer cells by using MTT assay. From the in vitro studies compound 8p, 8u and 8y were found most effective with an IC50 range of 0.56 -27.50 μM in MCF-7 and 2.57-36.54 μM in B16F10 cells.
Abstract: Aim : This clinical study aimed to evaluate the anti inflammatory efficacy of amla on plaque induced gingivitis.
Materials and Methods : This split mouth design study included 20 subjects diagnosed with plaque induced
gingivitis. The baseline gingival scores were recorded using gingival index (Loe and Sillness) after which
oral prophylaxis was done. Amla extract in gel form was applied in mandibular anterior sextant twice daily
for two weeks, at the end of which gingival scores were again recorded using the same scoring method and
compared with maxillary anterior sextant which acted as control.
Results : The data obtained was statistically analysed using unpaired t- test. Both maxillary and mandibular
sextants were compared at baseline and 2 weeks after the treatment. The results showed that there was
significant anti- inflammatory effect of amla 1 week after its application but no significant anti- inflammatory
effect of amla 2 weeks after its application on the inflamed gingiva.
Conclusion : Application of Amla gel showed significant reduction in the inflammation during the 1st week.
There was no significant improvement or deterioration in the gingival condition in the 2nd week of application.
Abstract: Anti-arthritic, anti-inflammatory and analgesic activity of combined extract of Annona
squamosa and Nigella sativa was evaluated and validated in various animal models. Arthritis
was induced by Complete Freund`s Adjuvant (CFA) injection in metatarsal footpad of
Sprague-Dawley rats. Degree of inflammation was evaluated by hind paw swelling and body
weight, estimation of AST, ALT and TP supported by histopathology of knee joint. Combined
extract reduced hind paw swelling, body weight, AST, ALT and TP Histopathology revealed
significant reduction in mononuclear infiltration, pannus formation and bone erosion.
Combined extract decreased the paw volume in carageenan treated rats. Combined extract
(PHF) shows moderate central and peripheral analgesic activities in hot plate method and
acetic acid induced writhing method in mice.
Abstract: Lipid-based formulations encompass a diverse group of formulations with very different physical appearance, ranging from simple tri-glyceride vehicles to more sophisticated formulations such as self-emulsifying drug delivery systems (SEDDS). Lipid-based drug delivery systems may contain a broad range of oils, surfactants, and co-solvents. They represent one of the most popular approaches to overcome the absorption barriers and to improve the bioavailability of poorly water-soluble drugs. Diversity and versatility of pharmaceutical grade lipid excipients and drug formulations as well as their compatibility with liquid, semi-solid and solid dosage forms make lipid systems most complex. Digestion of triglyceride lipids, physicochemical characteristics and solubilisation of lipid digestion products as well as intestinal permeability are some of the variable parameters of such formulations. Furthermore, among the factors affecting the bioavailability of the drug from lipid-based formulations are the digestion of lipid, the mean emulsion droplet diameter, the lipophilicity of the drug and the type of lipids. The solubility of the Active Pharmaceutical Ingredient in the Lipid System, the desorption /sorption isotherm and the digestibility of lipid vehicle are important issues to be considered for formulations of isotropic lipid formulations. This review also describes the fate of lipid formulations in the gut and the factors influencing the bioavailability from lipid-based formulations. Novel formulation systems and currently marketed product conclude this review.
Abstract: Purpose: To develop and characterize an oral extended-release matrix tablet of metformin
hydrochloride using a combination of a hydrophobic carrier and a hydrophilic polymer, and two types of
formulation techniques.
Methods: Various metformin hydrochloride formulations containing a hydrophobic carrier (stearic acid)
and a hydrophilic polymer (polyethylene oxide) were prepared using a 32 factorial design. Two types of
formulation techniques – melt granulation and direct compression – were evaluated. The influence of the
carrier, polymer and preparation method on metformin release from the formulations in vitro as well as
other physicochemical properties were studied. The release data were subjected to various release
kinetic models and also compared with those of a commercial brand.
Results: The physicochemical characteristics of all the granules and tablets were generally satisfactory.
Optimization results indicate that the release rate of metformin HCl was directly proportional to the levels
of stearic acid (SA) and polyethylene oxide (PEO) in the tablet formulations. Release rate was also
dependent on the method of granulation used. Kinetic analysis showed that the formulation containing
30 %w/w of polymer exhibited release similar to that of the commercial brand with a similarity factor (f2)
of 81.1. Melt granulation was more effective in extending drug release than direct compression. Release
mechanism followed most closely the Korsemeyer-Peppas model with a correlation coefficient (r2) and
0.991.
Conclusion: The use of a hydrophobic carrier along with a hydrophilic polymer effectively controls the
initial rapid release of a highly water soluble drug such as metformin HCl. Hot melt granulation method
was especially more effective in achieving this than the direct compression method.
Abstract: In current study, candesartan cilexetil was embedded in polyvinylpyrrolidone K30 matrix to produce solid dispersions by kneading method. The obtained granules
were incorporated into orally disintegrating tablets (ODTs). The tablets were developed by varying the ratios of superdisintegrants such as crospovidone and Ac-
Di-Sol. Incorporation of superdisintegrants strongly enhanced the dissolution rate of the highly lipophilic drug. The enhancement of dissolution rate strongly
depended on the type of superdisintegrants used and showed increase rate for crospovidone than Ac-Di-Sol. In addition, the increase in the dissolution behavior was
also contributed by the hydrophilic carrier. Therefore, oral disintegrating tablets based on polyvinylpyrrolidone K30 - crospovidone showed a much faster
dissolution than those based on polyvinylpyrrolidone K30 – Ac-Di-Sol. Finally, polyvinylpyrrolidone K30-crospovidone based solid dispersion tablets showed
excellent storage stability at 40 + 2oC /75 + 5% RH.
Abstract: The purpose of this investigation was to develop fast dissolving tablets (FDTs) of candesartan cilexetil by vacuum drying technique using camphor as subliming
agent. The prepared formulations were evaluated for pre-compressional and post-compressional parameters. The values of pre-compressional parameters were
within prescribed limits and indicated good free flowing properties. In all the formulations, the hardness test indicates good mechanical strength. Friability of all
formulations was less than 1. Drug content was found to be high (> 98%) and uniform in all the formulations. The tablet thickness was found to be 2.985– 3.148.
The weight variation results revealed that average percentage deviation was less then ± 5 %, which provides good uniformity in all formulations. The disintegration
time of the tablets found to be in the range of 25 to 69 sec. The formulations F3 and F6 released more than 90 % of the drug in 35 and 25 sec respectively. Amongst
all formulations, formulation F6 prepared by 7.5% camphor showed least disintegrating time of 25 sec and faster dissolution. Formulation F6 was then studied for
accelerated stability studies as per ICH guidelines for 60 days that shows no remarkable change in the formulation.
Abstract: Background: Hypertension shows circadian rhythm that there is a rise in pressure from the time of waking or before (about 4 to 8 a.m.), in most people. Conventional drug delivery system of captopril is inappropriate for the delivery of drug, as they cannot be administered just before the symptoms are worsened, because during this time the patients are asleep, bedtime dosing of captopril will not provide a therapeutic plasma drug concentration at the early hours of morning because of poor pharmacokinetic profile and shorter half-life of 1.9 hours. Thus, this study attempts to design and evaluate a chronomodulated pulsatile drug delivery system of captopril which was aimed to release the drug after a lag time of 6 hours. Materials and Methods: Present delivery system was prepared by rupturable coating method. The core containing captopril as a bioactive compound were prepared by direct compression method and then coated sequentially with an inner swelling layer containing hydrocolloid HPMC E5 and an outer rupturable layer consisted of Eudragit RL/RS (1 : 1). Total 12 formulations with different levels of inner swelling layer and outer polymeric layer were prepared and subjected to various processing and formulative parameters like the effect of core composition, level of swelling layer, and rupturable coating on lag time was investigated. In vitro drug release and rupture tests were performed using United States Pharmacopoeia paddle method at 50 rpm in 0.1N HCl and phosphate buffer of pH 6.8. Results: The results showed that as the amount of inner swelling layer increases, the lag time decreases and as the Eudragit coating level increases, the lag time increases and percent water uptake of time-dependent pulsatile release system decreases. The presence of an osmotic agent and effervescent agent helped in shortening of lag time. Conclusion: The system was found to be satisfactory in terms of release of the drug after the lag time of 6 hours.
Abstract: Aim:
The use of steroids concomitantly with antibiotics is common to treat the severe and destructive inflammation,
occurring during a bacterial infection of the external eye. In the present work, we have attempted to develop long
acting eye drops containing ciprofloxacin and dexomethasone, a potent antibiotic and anti-inflammatory agent in the
treatment of bacterial conjunctivitis.
Methods:
A clear ophthalmic solution and an ophthalmic suspension of the combination and ophthalmic solution of
Ciprofloxacin alone were prepared and evaluated by various tests.
Results:
The ophthalmic solutions formulated using the Hydroxypropyl-beta-cyclodextrin (HP-beta-CD) exhibited better
stability, biological activity and ocular tolerance in comparison to another ophthalmic preparation formulated without
hydroxypropyl-beta-cyclodextrin (HP-beta-CD).
Conclusions:
These eye-drops were found to be non-irritating to rabbit eyes and were found to be effective in prevention of
nonvascularisation in infected rabbit eyes.
Abstract: Pharmaceutical materials science being a fundamental branch that continuously
provides important insights, theories, and technologies to formulation sciences. The recent
advances in this area have brought the possibility to produce pharmaceutical materials by
design. In particular, the formation of co-crystals, i.e. crystalline molecular complexes of twoor
more neutral molecules, represents a potential route to achieve pharmaceutical materials with
improved properties of interest, including dissolution rate and stability under conditions of high
relative humidity. Co-crystals consists of API and a stoichiometric amount of a
pharmaceutically acceptable co-crystal former. Pharmaceutical co-crystals are nonionic
supramolecular complexes and can be used to address physical property issues such as
solubility, stability and bioavailability in pharmaceutical development without changing the
chemical composition of the API. These can be constructed through several types of interaction,
including hydrogen bonding, pi-stacking, and van der Waals forces. Phase transformations
induced during processing/storage affects the mechanisms of conversion of crystalline drugs to
co-crystals. Pharmaceutical co-crystals considered better alternatives to optimize drug
properties could play a major part in the future of API formulation and can be employed for
chiral resolution. This review introduces co-crystals as an emerging class of pharmaceutical
materials, focusing on the experimental methods applicable to their crystallization. In addition,
the examples illustrating how the co-crystal approach can be utilized to enhance the specific
properties of pharmaceutical solids, such as dissolution rate of poorly-water soluble APIs and
physical stability of moisture-labile APIs.
Abstract: Pulmonary drug delivery is a developing technology in which medication is inhaled through the lungs and enters the bloodstream through the alveolar epithelium. Pulmonary drug delivery provides a noninvasive, alternative method to subcutaneous injection, and also intravenous injection. The delivery device plays a major role in the efficiency of pulmonary delivery, and great strides have been made in the development of new devices in recent years. The devices most commonly used for respiratory delivery, including nebulizers, metered-dose inhalers, and dry powder inhalers, can all be adapted for use with protein/peptide drugs. The choice of device will depend on the drug, the formulation, the site of action, and the pathophysiology of the lungs. While a great deal of recent research has focused on the development of novel devices, attention must now be paid to the formulation of these macromolecular drugs. The emphasis in this review will be on targeting of drugs by inhalation using carriers (such as liposomes, microspheres, microparticles, and nanoparticles) and ligands.
Abstract: Solid lipid microparticles (SLMs) represent an alternative carrier system to traditional colloidal carrier such as
emulsion, liposomes and polymeric micro and nanoparticles. The purpose of this research work was to develop
and evaluate solid lipid microparticles of sirolimus for oral delivery. Sirolimus is an immunosupressive drug used to
prevent transplant rejection and to treat auto immune diseases. It is a macrolide lactone produced by streptomyces
hydroscopicus. It is extremely hydrophobic. Sirolimus solid lipid microparticles were prepared by hot homogenization
technique. The matrix chiefly consisted of glyceryl monostearate and sodium taurocholate. The SLMs were studied
for its particle size analysis, drug content, entrapment efficiency, in vitro release characteristics and also for stability
analysis at different temperature and humidity conditions. Average particle size was found to be 21.40μm. Drug
content of SLMs determined by HPLC analysis was found to be 98.6±0.31% while entrapment efficiency achieved
was 98.02%. Drug release from the final formulation was found to be 90.3% in 90 min. SLMs formulated with glyceryl
monostearate and sodium taurocholate can be used for oral delivery of hydrophobic drugs with in-vivo study still to
be explored.
Abstract: Purpose: Neostigmine bromide, a cholinesterase inhibitor is conventionally given by oral route for the treatment
of myasthenia gravis. However, it is very poorly absorbed from gastro-intestinal tract. Intranasal administration
is an ideal alternative to the parenteral route for systemic drug delivery. Formulating multiparticulate system with
mucoadhesive polymers may provide a significant increase in the nasal residence time. The aim of the present
approach was to overcome the drawbacks of the conventional dosage forms of Neostigmine Bromide by formulating
intranasal microspheres with Carbopol 974P NF and HPMC K15 M along with film forming polymer ethyl cellulose.
Methods: The microspheres were prepared by emulsion solvent evaporation method. The prepared
microspheres were characterized for encapsulation efficiency, drug loading, particle size, and surface morphology,
degree of swelling, in-vitro mucoadhesion, drug release, in-vivo studies and stability studies.
Results: Formulations IN1 and IN5 displayed the best results for Carbopol and HPMC based microspheres
respectively. Entrapment efficiency was 75.74±0.50% and 70.27±0.61%; mucoadhesion was 98.5% and 85.3%;
and drug release up to 8 h was 87.86% and 84.5% for IN1 and IN5 respectively. In-vivo studies revealed that the
formulations IN1 and IN5 showed good bioavailability compared to oral drug administration.
Conclusion: Both in-vitro and in-vivo studies conclude that Carbopol based microspheres are better than HPMC
based microspheres for the delivery of Neostigmine Bromide.
Abstract: Objective: To prepare and characterize Albumin microspheres of hydralazine hydrochloride for the treatment of
hypertension.
Methods: Albumin microspheres of antihypertensive drug hydralazine hydrochloride were prepared by emulsion
cross-linking method by using glutaraldehyde as cross-linking agent. Drug and polymer compatibility was determined by
Fourier-Transform Infrared spectroscopy. To determine the effect of polymer concentration and amount of glutaraldehyde,
formulations were characterized for their entrapment efficiency, particle size, surface morphology and release behavior.
In vivo study was carried out on hypertensive wistar rats.
Key findings: Maximum percentage entrapment efficiency (%EE) was found to be 68.20±1.03 %. Laser particle
size analyzer confirmed mean particle size in the range of 31.7 to 39.6μm. In vitro drug release studies showed a
biphasic release pattern for all formulations with an initial burst effect followed by slow release for almost 24 hrs.
Conclusion: In vivo study to determine antihypertensive effect of selected formulation strongly correlates with in
vitro drug release behavior. The release behavior was significantly regulated by polymer concentration and volume of
glutaraldehyde. The study revealed that hydralazine hydrochloride loaded albumin microspheres exhibited prolonged
reduction of systolic and diastolic arterial pressure compared to hydralazine hydrochloride solution.
Abstract: Purpose:
The use of steroids concomitantly with antibiotics is common to treat the severe and destructive
inflammation, occurring during a bacterial infection of the external eye. In the present work, we have
attempted to develop eye drops containing ciprofloxacin and dexomethasone, a potent antibiotic and
anti-inflammatory agent in the treatment of bacterial conjunctivitis.
Methods:
A clear ophthalmic solution and an ophthalmic suspension of the combination were prepared and
evaluated by various physicochemical, microbiological and biological tests.
Results:
The magnitude i.e. drug concentration in aqueous humour obtained after application of the various types
of the preparation were in order conventional solution> aqueous gel >ointment.
Conclusions:
A combination of ciprofloxacin and dexamethasone was developed for the first time, in the form of eyedrops,
as a clear solution and a suspension. The formulations were simple and prepared relatively easily.
In both the formulations, dexamethasone was found to be stable at and below temperatures of 25oC. At
higher temperature it showed considerable degradation. These eye-drops were found to be non-irritating
to rabbit eyes and were found to be effective in prevention of nonvascularisation in infected rabbit eyes.
Abstract: The effects of prophylactic administration of extracts of bark of
Sesbania grandiflora and fruit of Terminalia chebula on the development of
carrageenan induced paw oedema and adjuvant - induced arthritis to assess
influence of high NO level in the form of exogenous herbal extracts of bark of
Sesbania grandiflora (300 mg/kg b.w.) and fruit of Terminalia chebula (500
mg/kg b.w.) in the progress of inflammation and polyarthritis. Inflammation
was assessed by measuring paw swelling. was significantly reduced after
prophylactic administration of extracts of bark of Sesbania grandiflora (300
mg/kg b.w.) and fruit of Terminalia chebula (500 mg/kg b.w.). Arthritis was
assessed by measuring paw oedema , spleenomegaly, thymic involutions and
loss in body wt. which are features of adjuvant- induced arthritis were
effectively reduced after prophylactic administration of extracts of bark of
Sesbania grandiflora (300 mg/kg b.w.) and fruit of Terminalia chebula (500
mg/kg b.w.). These data suggests that high NO level in the from extracts of bark
of Sesbania grandiflora and fruit of Terminalia chebula may suppress initial
stages of immune response to carrageenan and adjuvant injection probably by
inhibiting iNOS expression through feedback inhibition mechanism and
showed potent anti-inflammatory and anti-arthritic activity.
Abstract: An orodispersible dosage form has been developed as a user-friendly formulation that disintegrates in the mouth
immediately. Thus an attempt was made to improve the onset of action of bronchodilator used commonly in the
treatment of asthma. Formulation was optimized for type of disintegrant used and method of formulation. Disintegrants
such as CCS (Croscarmellose Sodium), SSG (Sodium Starch Glycolate), L-HPC (Low-substituted Hydroxy Propyl
Cellulose), and Crospovidone XL-10 were used and tablets were prepared by direct compression method and wet
granulation. Wet granulation formulation were again sub-divided where disintegrant was added intragranularly in one
type and was added both in intra and extra granulation in the other. Mint flavor was added to give good mouth feel.
Out of all formulations prepared, the one prepared with Crospovidone XL-10 added both intra and extra granulation
showed least disintegrating time (9 sec) with good flow property. Direct compression blends had poor flow. Tablets
were also evaluated for various physicochemical parameters. All the tablets showed burst release of drug. Hence,
it was concluded that out of all formulations, the one prepared with Crospovidone XL-10 added both intra and extra
granulation was the best formulation as it showed the least disintegration time.
Abstract: In the present work an attempt was made to formulate and evaluate a sustained release implant of
tramadol HCl using biodegradable polymer Chitosan. Implants of tramadol were prepared by extrusion method
using specially designed extruder with biodegradable naturally occurring polymer chitosan. Tramadol
hydrochloride (TRH), a centrally acting opioid analgesic, is used in severe acute or chronic pains. It offers
several therapeutic advantages over other analgesics, such as good bioavailability and elimination half-life (5–7
h). Despite the long elimination half-life, TRH is prescribed 3–4 times a day. These properties make the
tramadol an ideal drug candidate for implantable controlled drug delivery. Since the release of tramadol from
chitosan was spread over a period of 1 to 8 days by varying the concentration of polymer and Crosslinking
time, these implants could be used for pain management such as carcinomas, post operative surgery,
osteoarthritis, by suitable modification in the formulae, or in the drug release from implants.
Abstract: Objective: The objective of the present study was to study the in vitro and in vivo release pattern of a drug from Ciprofloxacin ophthalmic formulations for the treatment of bacterial conjunctivitis.
Methods: Three different formulations of Ciprofloxacin were prepared, viz. conventional solutions, aqueous polymeric gel and hydrophobic ointment and evaluated for in vitro and in vivo release. In the vivo studies carried out in healthy rabbits, the highest drug levels were obtained with the gel, followed by the conventional solution and lowest with the ointment.
Results: In the in vivo studies, it was found that a single dose of the gel produced highest drug concentrations in the aqueous humour. The conventional solution could produce high concentrations on repeated dosing only. The ointment on the other hand produced very low levels due to its hydrophobic nature.
Conclusion: The gel can be successfully used to prolong the duration of action of ciprofloxacin and also provide high intraocular concentrations, as compared to the conventional solution and the ointment. These eye-drops were found to be non-irritating to rabbit eyes and were found to be effective in prevention of non-vascularization in infected rabbit eyes.
Abstract: he aim of present study was to prepare and characterize biphasic release tablet formulation containing Metformin HCl in extended release matrix form and Pioglitazone HCl in immediate release form for the treatment of diabetes mellitus. Different formulations containing Metformin HCl were manufactured using 32 factorial designs. Influence of hydrophobic carrier, hydrophilic polymer on drug release was studied. Immediate release layer of Pioglitazone was optimized using different disintegrants. All formulations were evaluated for % drug release and analyzed according to various release kinetic models. Optimization results indicated that release rate of Metformin is directly proportional to the levels of stearic acid and Hydroxypropyl methylcellulose. Kinetic analysis showed that formulation F5 was good releasing with f2 value of 85.34 and follows Higuchi and peppas model with correlation coefficient value 0.9929 and 0.9924 respectively. Similarly optimization study indicated that release of pioglitazone is dependent on the level and type of disintegrant, formulation P5 shown highest f2 value of 84.08. Results confirmed that biphasic release tablet formulation containing extended release of Metformin HCl and immediate release of Pioglitazone HCl can be developed for the treatment of diabetes mellitus.
Abstract: A major hurdle in pharmaceutical formulation is water insolubility of most of the drugs affecting stability and
bioavailability of the drug, if the drug is also insoluble in organic medium, it is difficult to deliver the drug in a sufficiently
bioavailable form and hence it is a great challenge to formulation researchers to overcome such difficulty. Although
some approaches are available for enhancing the dissolution of poorly soluble drugs but has certain draw backs like
low drug loading and large doses. However, a new solution to poorly water soluble drug candidates is now available i.e.
nanonisation and it leads to much more soluble, more biologically available and safer dosage form of poorly soluble and
poorly bioavailable drugs. In the present work, a nanocrystal of lovastatin was formulated by using simple precipitation
method without using stabilizer or surfactant and it was found that formulation at 3 mM concentration of drug with the
acetone and methanol as a solvent and at proper dilution (50 times) of drug solution with water, nanocrystals with less
particle size is possible with slight change in crystallinity. It has also shown that, the drug has enhanced saturation
solubility, increased dissolution rate and more bioavailable in biological fluid when drug formulated by using acetone
and methanol as a solvent. Whereas drug formulation with acetonitrile has large particle size, less saturation solubility
and low rate of dissolution.
Abstract: In the present study we have examined the effects of prophylactic
administration of extracts of bark of Sesbania grandiflora and Sesbania
sesban on the development of carrageenan induced paw oedema and
adjuvant - induced arthritis to assess influence of high NO level in the
form of exogenous herbal extracts of bark of Sesbania grandiflora
and Sesbania sesban in the progress of inflammation. Inflammation
was assessed by measuring paw swelling. Increased paw oedema of
the injected paw measured on 1st to 12th hrs which is feature of
carrageenan induced inflammation was significantly reduced after
prophylactic administration of petroleum ether, chloroform and methanol
extracts of bark of Sesbania grandiflora (300mg/kg b.w. p.o.) and
Sesbania sesban (300mg/kg b.w. p.o.) and arthritis was assessed by
measuring primary and secondary paw swelling and changes in thymus,
spleen and body weight. Increased swelling of the non injected paw
(secondary paw) measured on days 14 and 21, injected paw swelling
(primary paw) measured on days 3, 14 and 21, spleenomegaly, thymic
involutions and loss in body wt. which are features of adjuvant- induced
arthritis were effectively reduced after prophylactic administration of
extracts of bark of Sesbania grandiflora and Sesbania sesban . We
have also claimed that exposure to extracts of Sesbania grandiflora
and Sesbania sesban during inflammation process may be modulate
the inflammation process due to presence of the isolated triterpenoidal
compounds.
Abstract: The present study was carried out to investigate the effects of Polyherbal extract (PHE) on liver fibrosis in rats induced by carbon tetrachloride (CCl4) and to explore its possible mechanisms. Liver injury was induced in Male Wistar albino rats by injection with 50% CCl4 subcutaneously twice a week for 8 weeks. At the same time, Polyherbal extract (50, 100 and 150 mg/kg) was administered intragastrically. Upon pathological examination, the Polyherbal extract-treated rats significantly reduced the liver damage and the symptoms of liver injury. Administration of Polyherbal extract (PHE) decreased CCl4-induced elevation of serum transaminase activities, hyaluronic acid, laminin and procollagen type III levels, and contents of hydroxyproline in liver tissue by approximately 30–60%. It also restored the decrease in SOD and GSH-Px activites and inhibited the formation of lipid peroxidative products during CCl4 treatment. Moreover, Polyherbal extract (100, 150 mg/kg, ig) decreased the elevation of TGF-β1 by 47.7% and 53.1%, respectively.These results suggested that Polyherbal extract significantly inhibited the progression of hepatic injury induced by CCl4, and the inhibitory effect of Polyherbal extract on hepatic injury might be associated with its ability to scavenge free radicals, decrease the level of TGF- β1.
Abstract: This study was undertaken to investigate the effect of Polyherbal formulation of Annona squamosa and Nigella sativa on blood glucose, plasma insulin, tissue lipid profile, and lipidperoxidation in streptozotocin induced diabetic rats. Aqueous extract of Polyherbal formulation of Annona squamosa and Nigella sativa was administered orally (200 mg/kg body weight) for 30 days. The different doses of Polyherbal formulation on blood glucose and plasma insulin in diabetic rats were studied and the levels of lipid peroxides and tissue lipids were also estimated in streptozotocin induced diabetic rats. The effects were compared with tolbutamide. Treatment with Polyherbal formulation and tolbutamide resulted in a significant reduction of blood glucose and increase in plasma insulin. Polyherbal formulation also resulted in a significant decrease in tissue lipids and lipid peroxide formation. The decreased lipid peroxides and tissue lipids clearly showed the antihyperlipidemic and antiperoxidative effect of Polyherbal formulation apart from its antidiabetic effect.
Abstract: A method is presented for selecting a polyvinyl alcohol as a stabilizing agent for suspension
polymerization without carrying out the polymerization reaction. This method is
demonstrated for polymerization of water- insoluble and water-soluble monomers. Here the
stability of the non-reacting suspension is used to predict the stability of the same system,
when it is reacting.
Abstract: Purpose: To investigate the production of antibiotic from actinomycetes isolated from soil and evaluate
its antimicrobial activities.
Methods: In a medium formulation study, A-4 and A-4 actinomycete mutant strains (out of the six
strains selected from the nine actinomycetes that were screened) were evaluated for maximum
antibiotic production using various carbon and nitrogen sources. Zone of inhibition and packed cell
volume were the parameters used for the evaluation. Various fermentation conditions such as pH,
temperature and dissolved oxygen were also optimized for maximal production of antibiotic from both A-
4 and A-4 mutant.
Results: Some actinomycetes strains showed promising antimicrobial activity against different strains of
bacteria and fungi. Out of the six strains selected, one strain, designated A-4, showed maximum
antimicrobial property against Gram positive and Gram negative strains as well as against various fungi.
Conclusion: Findings from this investigation reveal that strain A-4 and A-4 mutant strains, in that order,
exhibited superior antimicrobial activities to other soil isolates of actinomycetes.
Abstract: Purpose: Two critical factors that govern the stability of pharmaceutical formulations in the tropics are
humidity and temperature. This study was carried out to investigate the effect of moisture sorption at two
different storage conditions on Cefaclor dry powder for oral suspension and predict the effect of
moisture interaction on the reconstituted formulations
Method: Cefaclor dry powder for suspension formulation was taken as a model formulation for this
study. Different formulations were manufactured and placed in twelve amber coloured glass bottles for
each test condition. One set of bottles was sealed by heat induction technique under vacuum to ensure
the integrity of the seal while the other set was without a seal but had a child-resistant cap. Both types of
bottles were stored in humidity chambers at 30°C/65%RH or 40°C/75%RH. Weight changes were
monitored on a dynamic moisture balance over a period of 3 months.
Results: The results were recorded in terms of moisture content, colour, and excipient interaction and
their effect on product appearance. The data were analyzed using Students t-test and one way analysis
of variance (ANOVA), and differences were considered statistically significant at P < 0.05.
Conclusions: The study revealed that the product with enhanced packaging and also contained nonwater
soluble colourants were more protected against the deleterious effects of moisture and
temperature. The findings provide an insight into a possible approach for formulating moisture-sensitive
pharmaceutical products, especially dry powder preparations for use in the tropics.
Abstract: The present study was designed to evaluate targeting efficiency of carboplatin anticancer drug. Drug was encapsulated in natural biodegradable polymer sodium alginate. The nanoparticles were prepared by the ion gelification technique and evaluated for encapsulation efficiency, loading capacity, in vitro release pattern and targeting efficiency. Drug encapsulation efficiency was about 52.24–68.70% for different formulations. In vitro release profile showed duration of drug release was also increased (more than 12 h) by nanoparticulate formulation as compared to pure drug (up to 3 h). The formulations were parenterally administered to laca mice and the drug was detected in body organs like liver, lungs and spleen. In case of free drug, less amount of drug was found in liver, lungs and spleen as compared to drug encapsulated nanoparticles. Thus sodium alginate nanoparticles can be used for targeting carboplatin and it can be a promising tool in the delivery of anticancer drugs.
Abstract: Purpose: To isolate and Characterize the antibiotic producing actinomycete.
Methods: Crowded plate technique was used for the isolation of actinomycetes using media like soybean – casein digest medium actinomycetes isolation agar. The morphological and cultural characterization of one of the selected strain designated as A-4 was performed as per International Streptomycete Project described by Shirling and Gottlib.
Results: Morphological and cultural studies showed that the A-4 is belonging to actinomycete genus. The morphological and cultural characteristics of A-4 mutant showed cellular and aerial growth as well as soluble pigment formation in various ISP media.
Conclusion: The findings from this investigation revealed that the selected strain A-4 is actinomycete.
Abstract: In screening of new antibiotics, several actinomycetes were isolated from
soil samples. Crowded plate technique was used for the isolation of
actinomycetes. The morphological and cultural characterization of A-4
strain was performed. In medium formulation study for A-4 and A-4 mutant,
various carbon and nitrogen sources were tested for maximum antibiotic
production using zone of inhibition and packed cell volume (%) as
parameters. Various fermentation conditions like pH, temperature and DO2
were also optimized for the maximal production of antibiotic from both A-4
and A-4 mutant. All medium formulation as well as bioprocess parameters
for A-4 and A-4 mutant strains was compared. Some actinomycetes
strains, showed promising antimicrobial scores against different strains of
bacteria and fungi. From the six strains selected, one strain designated as
A-4 showed maximum antimicrobial property against gram positive and
gram negative strains as well as various fungi. Morphological and cultural
studies showed that A-4 is belongs to actinomycete genus.. The strain A-4
and A-4 mutant was found to be having better antimicrobial activity in
comparison with other soil isolates of actinomycetes.
Abstract: Amino-benzothiazoles constitute an important class of compounds. In recent year heterocyclic
compounds analogues and derivatives have attracted strong interest due to their useful biological
and pharmacological properties. The small and simple benzothiazole nucleus is present in
compounds involved in research aimed at evaluating new products that possess biological
activities, such as anti-tumor, anti-microbial, anthelmintic, anti-leishmanial, anti-convulsant and
anti-inflammatory. The present review focuses on the different methods of the substituted
benzothiazoles with potential activities that are now in development.
Abstract: The present study is aimed to evaluate the leaf extracts of Gymnema sylvestre for acclaimed
anti-arthritic activity using albino rats. The arthritic action of leaves of Gymnema sylvestre
was studied in Freund's adjuvant induced arthritis in rats. Diclofenac sodium was used as a
standard drug. The study revealed that the petroleum ether (40—60°) extract and aqueous
extract of Gymnema sylvestre possessed significant anti-arthritic activity in all parameters of
the study compared to control group. The more potent anti-arthritic activity of leaves of
Gymnema sylvestre may be due to nature of steroids, triterpenoids and saponin glycosides.
This claim demands further detailed phytochemical profile to identify the active constituent
responsible for the anti-arthritic activity.
Abstract: Nitric Oxide (NO) can autoregulate its own formation by feedback inhibition of the
inducible Nitric Oxide Synthase (iNOS). Modulation of biosynthesis or activity of NO
results in amelioration if pathogenesis of experimental arthritis. However, little is known
about feedback mechanism on NO generation in response to carrageenan induced paw
oedema and adjuvant- induced arthritis. In the present study we have examined the
effects of prophylactic administration of extracts of bark of Sesbania grandiflora and
Sesbania sesban on the development of carrageenan induced paw oedema and adjuvant
- induced arthritis to assess influence of high NO level in the form of exogenous herbal
extracts of bark of Sesbania grandiflora and Sesbania sesban in the progress of
inflammation. Inflammation was assessed by measuring paw swelling. Increased paw
oedema of the injected paw measured on 1st to 12th hrs which is feature of carrageenan
induced inflammation was significantly reduced after prophylactic administration of
petroleum ether, chloroform and methanol extracts of bark of Sesbania grandiflora
(300mg/kg b.w. p.o.) and Sesbania sesban (300mg/kg b.w. p.o.) and arthritis was
assessed by measuring primary and secondary paw swelling and changes in thymus,
spleen and body weight. Increased swelling of the non injected paw (secondary paw)
measured on days 14 and 21, injected paw swelling (primary paw) measured on days 3,
14 and 21, spleenomegaly, thymic involutions and loss in body wt. which are features of
adjuvant- induced arthritis were effectively reduced after prophylactic administration of
extracts of bark of Sesbania grandiflora and Sesbania sesban . These data suggests that
high NO level in the from extracts of Sesbania grandiflora and Sesbania sesban may
suppress initial stages of immune response to carrageenan and adjuvant injection
probably by inhibiting iNOS expression through feedback inhibition mechanism.
However, further studies are required to unravel the mechanism involved in these
effects of extracts of bark of Sesbania grandiflora and Sesbania sesban and their clinical
implications.
Abstract: Oral route of administration have wide acceptance up to 50-60% to total drug forms. Fast disintegrating drug delivery system has number of advantage such as faster onset of action, attractive elegance, ease of administration. In this study, an attempt has been made to study direct compression method, for formulation of fast disintegrating tablets of Rifampicin, an anti-tubercular drug in view of enhancing bioavailability. These formulations have sufficient hardness and can be manufactured by commonly used equipment. Prior to formulation the pre compression parameters were characterized for flow properties and prepared formulations were evaluated for physico-chemical parameters, X-ray powder crystallography, SEM. All four formulations possessed good disintegration properties with total disintegration time of 25 to 40 seconds. The effects of different superdisintegrants and process variables on drug release profile and disintegration
property were evaluated and results revealed the better drug release with different superdisintegrants such as Ac-di sol, Explotab, Kollidon CL and Polyplastadone XL. All formulations are rapidly disintegrated in oral cavity as well as all formulations possess good antitubercular properties. SEM Showed the mechanical strength of the formulations affected the morphological changes after compression. Hence, it is evident from this study that fast dispersible tablets could be a promising delivery system for Rifampicin with good mouth feel and improved drug availability with better patient compliance.
Abstract: The current work aims to investigate the sudden drop of dissolution with respect to higher compression pressure and hardness of tablet with a good and comparative less significant disintegration time and to understand an affect of pressure on drug with respect to compression behavior on dissolution and other properties. Where Cefuroxime Axetil was compressed at different pressure in form of pellets and tablets using hydraulic press and compression machine respectively, and characterized to understand any physical and chemical change using X-ray powder diffraction, differential scanning calorimetry, Dissolution and Scanning Electron microscopy. Scanning electron microscopy studies of pellets revealed that the change in surface morphology from opaque to translucent clear with increase in breaking force, these different pressure compressed pellets were subjected to uniform reduction of particle size. The similarity factor f2 values of drug release profile were comparably same. The breaking force and pellet hardness had indicated a very firm intrinsic binding force exist with Cefuroxime Axetil, study had investigated the decrease in-vitro dissolution is marked by the compact binding property of individual particles of Cefuroxime Axetil between the excipient due to the increase in compression force.
Abstract: A major hurdle in pharmaceutical formulation is water insolubility of most of drugs
affecting their stability and bioavailability. If the drug is also insoluble in organic
medium, it is difficult to deliver it in a sufficiently bioavailable form and hence it
is a great challenge to formulation researchers to overcome such difficulty. Although
some approaches are available for enhancing the dissolution of poorly soluble
drugs, there has been certain draw backs like use of organic solvents, low drug loading
and large doses. However, a new solution to poorly water soluble drug candidates
is now available, i.e. nanonisation that leads to much more soluble, more biologically
available and safer dosage form of poorly soluble and poorly bioavailable drugs.
Controlled release of these drugs is also possible by forming nanostructured
matrices. In this article, a brief description of production methods of drug
nanoparticles and commercialized methods are presented along with brief overview
on second generation of drug nanocrystal (Smart crystal technology), controlled
release of hydrophobic drugs and recent works thereof are also presented.
Abstract: Gatifloxacin ocular films were prepared by solvent casting method using hydroxy propyl methyl cellulose, methyl cellulose, sodium carboxy methyl cellulose and gelatin in different concentrations using glycerin as plasticizer. The physicochemical parameters of the ocular films were evaluated. The compatibility of the drug in the formulations was confirmed by IR studies. In vitro diffusion studies and mechanism of drug release was identified. The formulation F4 and F8 shows a maximum cumulative percentage drug release of 96.15 % and 97.34 % at the end of 12th h respectively. The drug release decreases in all the formulations as the concentration of polymer increases. The release of drug from the films has followed first-order kinetics and non-fickian in nature with diffusion controlled mechanism. The formulation F4 and F8 were subjected to UV-irradiation and in vivo drug release studies on rabbits. A high correlation coefficient was found between in vitro and in vivo release rate studies. No significant change in the drug content and physical features was observed during storage at 30±2°C/65±5% RH and 40±2°C/75±5% RH for three months. The data demonstrated that hydroxy propyl methyl cellulose and methyl cellulose in the concentration of 4.5% w/v was suitable for developing sustained release ocular films of gatifloxacin.
Abstract: This review on the gene therapy describes about DNA and it’s function. It further contains the description on gene therapy along with it’s definition. Various approaches for gene therapy have been described in this paper. The genetic disorders and the use of gene therapy for these diseases have been discussed along with the methods that can be used for gene delivery. Vector and non-Vector methods can be used for gene therapy. For vector method retroviral method, herpes simplex vectors can be used for gene therapy. Whereas for non-vector method molecular conjugates, naked DNA can be used for the same purpose. Further the paper contains a note on the gene therapy for curing disorders like Ischemic stroke, cancer. Few case studies of setbacks and achievements for gene therapy have been discussed at last.
Abstract: This paper describes the formulation andevaluation of transdermal patches of OndansetronHydrochloride. The films were formulated usingdifferent hydrophilic and lipophilic polymerscombination of hydrophilic-lipophlic polymers,ethyl cellulose : poly vinyl pyrrolidine. Thepolymeric films of Ondansetron Hydrochloridewere prepared using film casting technique onmercury substrate. The study is also extended toinvestigate the effect of plasticizer such as dibutylphthalate and propylene glycol and effect ofpenetration enhancer oleic acid by using kesharycheindiffusion cell. The films were evaluated forphysico-chemical properties. In vitro drugdiffusion study through rat skin indicateshydrophilic polymer showed higher release thanthe liphophilic and hydrophilic-lipophiliccombination. The release rate was found to followfirst order kinetics. Also permeation enhancerwas found to give favourable permeationenhancement.
Abstract: Context: Transdernal delivery of drugs through the skin to the systemic circulation provides a convenient route of administration for a variety of clinical indications.
Objective: To develop a matrix-type transdermal therapeutic system containing diltiazem HCl with different ratios of hydrophilic and hydrophobic polymeric combinations.
Materials and Methods: Transdermal patches were prepared by the solvent evaporation technique with the aid of oleic acid and tween 20 as permeation enhancers using Eudragit RL 100 and PVP as hydrophilic polymers and Ethyl cellulose as hydrophobic polymer. The formulations were subjected to various physicochemical studies, in vitro drug permeation studies using pretreated cellophane paper and a human cadaver skin.
Results and Discussion: The results showed that the release of drug followed the Higuchikinetics (r2=0.997-0.999), and the mechanism was diffusion mediated. The results from the stability studies indicate that the selected formulations were stable.
Conclusion: The drug loaded polymeric films composed of D3 [EC:PVP (7.5:2.5)] and D6 [ERL 100:EC (8:2)] with 5% Tween 20 as permeation enhancer might be selected for manufacturing transdermal patch by using a suitable adhesive layer and backing memberane with in vivo performance of the films remained to be studied.
Abstract: A simple and accurate Reverse Phase High-Performance Liquid Chromatography (RPHPLC) method was developed to determine Etamsylate in injection formulations. The drug was chromatographed on a reversed phase C-18 column. Eluents were monitored at a wavelength of 220 nm using a mixture (40:60) Methanol: Buffer (phosphate buffer). Solution concentrations were measured on weight basis to avoid the use of an internal standard. The method was spastically validated for linearity, accuracy, precision and selectivity. Due to its simplicity and accuracy, method will be useful for routine quality control analysis.
Abstract: Solventless compression coating was one of the strategies for delivering drugs to the colon based on gastrointestinal pH and transit time concept. The present study was aimed to develop rapidly disintegrating diclofenac sodium core tablets compressionâ€coated with a mixture of time dependent hydrophilic swellable polymer hydropropylmethylcellulose (HPMC) and pH responsive soluble polymer Eudragit® S 100 (ED) in different ratios. The effect of proportion of HPMC and ED in the coat on premature drug release in upper part (stomach and small intestine) of gastrointestinal tract and the amount of drug release in colon target area was studied. It was found that core tablets compressionâ€coated with HPMC and ED alone fails to prevent drug release in upper part of gastrointestinal tract and release was incomplete in the colon target area from HPMC compressionâ€coated tablets, where as drug release was not sustained in colon from ED compressionâ€coated tablets. The formulations released 1.24% to 6.82% of drug in physiological environment of stomach and small intestine depending upon proportion of HPMC and ED in the coat. The core tablets compressionâ€coated with HPMC and ED mixture in the ratio 6:4 was found to be suitable for targeting diclofenac sodium to the colon owing to its minimal drug release in physiological environment of stomach and small intestine and releases 92% of drug in the target area. The presence of ED in hydrophilic compression coat retarded the initial swelling of the coat in acidic to weakly acidic pH, but in alkaline pH, enhancement in drug release rate was observed due to the dissolution of ED from the coat with time resulting in a porous coat structure, resulted in a faster and controlled drug release in the target area.
Abstract: Purpose: Most eye diseases are treated with topical application of eye drops. The poor bioavailability and therapeutic response exhibited
by these conventional eye drops due to rapid precorneal elimination of the drug may be overcome by the use of in situ gelling systems
that are instilled as drops into the eye and undergo a sol-to-gel transition in the cul-de-sac. Hence, the purpose of the present work was to
formulate and evaluate an ophthalmic delivery system for a nonsteroidal anti-infl ammatory drug, ketorolac tromethamine, based on the
concept of pH-triggered in situ gelation. Methods: Polyacrylic acid (Carbopol® 934) was used as the gelling agent in combination with
hydroxypropylmethylcellulose (Methocel K4M) which acted as a viscosity enhancing agent. Compatibility studies of the drug excipients
were carried out using differential scanning calorimetry (DSC). The prepared formulations were characterized for clarity, pH, drug
content, sol-to-gel transition by scanning electron microscopy (SEM), in vitro and in vivo drug release, ocular irritation and stability.
Results: The clarity, pH and drug content of the developed formulation were found to be satisfactory. The developed formulation
was therapeutically effi cacious, stable, non-irritant, and provided sustained drug release over an 8-h period. The formulation with
benzalkonium chloride and edetate disodium improved the rate of corneal absorption but not the extent. Conclusions: The developed
formulation is a viable alternative to conventional eye drops by virtue of its ability to enhance bioavailability through its longer
precorneal residence time and ability to produce sustained drug release. Also important factor is the ease of instillation and the reduced
frequency of instillation resulting in better patient acceptance.
Abstract: The alcoholic extract of Gymnema sylvestre leaves was investigated for evaluation of Wound healing properties in rats at a dose 200 mg/kg. Results of in-vivo activity lead to the conclusion that the alcoholic extract of Gymnema sylvestre showed significant wound healing properties by excision, incision and dead space granuloma models.
Abstract: Most ocular diseases are treated with topical eye drops. The poor bioavailability and
therapeutic response exhibited by these conventional eye drops due to rapid precorneal elimination of the
drug may be overcome by the use of in situ gelling systems that are instilled as drops into the eye and
undergo a sol-to-gel transition in the cul-de-sac. The present work describes the formulation and
evaluation of an ophthalmic delivery system of the nonsteroidal anti-inflammatory drug (NSAID),
ketorolac tromethamine, based on the concept of pH-triggered in situ gelation. Polyacrylic acid
(Carbopols 934) was used as the gelling agent in combination with hydroxypropylmethylcellulose
(Methocel E15LV), which acted as a viscosity enhancer. The prepared formulations were characterized for
clarity, pH, drug content, rheology, and in vivo drug release. Clarity, pH, and drug content of the
developed formulations were found to be satisfactory. The developed formulation showed pseudo-plastic
rheology. The formulation with benzalkonium chloride and edetate disodium improved the rate of corneal
absorption but not the extent. The developed formulation is a viable alternative to conventional eye drops
by virtue of its ability to enhance bioavailability through its longer precorneal residence time and ability to
sustain drug release. Also importantly is the ease of instillation afforded and decreased frequency of
instillation resulting in better patient acceptance. Drug Dev Res 69:1–8, 2009. r 2009 Wiley-Liss, Inc.
Abstract: Dendrimers are new class of polymeric materials. It is generally described as a macromolecule, which is characterized by its extensively branched 3D structure that provides a high degree of surface functionality and versatility. The unique properties associated with these dendrimers such as uniform size, high degree of branching, water solubility, multivalency, well-defined molecular weight and available internal cavities make them attractive for biological and drug-delivery applications. Commercialization of dendrimers is now forthcoming. The present review briefly describes about dendrimer synthesis strategies, types of dendrimers with different functionalities, properties which having crucial importance and their potential applications.
Abstract: Many patients find it difficult swallow tablets and hard gelatin capsules and don't take their medication as prescribed. it is estimated that 50% of the population is affected by this problem which results in a high incidence of non-compliance and ineffective therapy. The difficulty is experienced particularly by paediatric and geriatric patients, but it also applies to people who are ill in bed and those active working patients who are busy or traveling, especially those who have no access to water. To improve patient compliance, fast dispersible tablets have emerged as an alternative to conventional oral dosage forms. Freeze-drying, sublimation, spray drying, disintegrate addition, tablet molding and use of sugar-based excipients are the techniques, the aim is to the formulation of fast dispersible tablets. Despite the different mechanisms involved in these techniques, the aim is to provide the tablet that quickly disintegrates or dissolves upon contact with saliva and also provides better patient compliance.
Abstract: The invention relates to controlled drug delivery formulations for parenteral administration of active agent. The controlled drug
delivery formulations in the form of microspheres are developed for parenteral administration of antihypertensive agent. The
controlled drug delivery formulations developed in the form of albumin microspheres for intramuscular administration of Hydralazine HCl to give during emergency and to avoid complications associated via other routes and with a view of giving a prolonged release of the Hydralazine HCl. Microspheres were prepared with natural polymer BSA using emulsion polymerization technique or emulsion cross-linking method. The prepared microspheres proved to be a potential candidate for microparticulate parenteral controlled drug delivery system.
Abstract: Immune system dysfunction is responsible for various diseases like arthritis, ulcerative colitis, asthma, allergy, parasitic diseases, cancer and infectious diseases. In clinical immunology laboratory tests, which utilize a great many of the recently elucidated principles of immunology can be performed. The results are then used by practicing physicians in the diagnosis, treatment and prognosis of the clinical disorders. Further more, qualitative and quantitative analysis of immune response has led to better understanding of pathogenesis of many clinical disorders. These understanding in turn have stimulated further basic scientific research in immunology. The degree to which the patient becomes abnormally susceptible to infections by this microbial environment depends on the extent of immunosuppression. For that the immunomodulatory study of the leaves Gymnema Sylvestre R.Br.(Asclepiadaceae) was carried out by in-vitro. The aqueous extract of Gymnema Sylvestre leaves was investigated for immunomodulatory activity by assessing Neutrophil locomotion and chemotaxis test, phagocytosis of killed Candida albicans and Nitroblue tetrazolium test. The extract was given at dose of 25µg/ml, 50µg/ml and 100µg/ml. Result of in-vitro immunomodulatory activity lead to the conclusion that the aqueous extract of Gymnema Sylvestre showed predominantly significant activity on in-vitro human neutrophils in all parameters, which is compared to the standard.
Abstract: Some new 2-Amino substituted- benzothiazole (A1-7) were synthesized by treating with KSCN in presence of glacial acetic acid and
with different Substituted aniline. Structures of the synthesized compounds were established on the basis of Melting Point, TLC, and IR
spectral data. The anti microbial activity of the synthesized compounds was evaluated by disc diffusion method.
Abstract: Some new 2-Amino substituted- benzothiazole (A1-7) were synthesized by treating with KSCN in presence of glacial acetic acid and with different Substituted aniline. Structures of the synthesized compounds were established on the basis of Melting Point, TLC, and IR spectral data. The anti-fungal activity of the synthesized compounds was evaluated by disc diffusion method.
Abstract: In recent year heterocyclic compounds analogues and derivatives have attracted strong interest due to their useful biological and pharmacological
properties. The small and simple benzothiazole nucleus is present in compounds involved in research aimed at evaluating new
products that possess biological activities, such as anti-tumor, anti-microbial, anthelmintic, anti-leishmanial, anti-convulsant and anti-inflammatory.
The present review focuses on the benzothiazoles with potential activities that are now in development.
Abstract: The invention relates to nanocrystals of poorly water soluble drugs to increase their solubility and dissolution rate and thereby
increased bioavailability. It specifically relates to the preparation of statin nanocrystals. More particularly it relates to the easy and
cost-effective process for preparation of lovastatin nanocrystals and its formulations for convenient oral delivery. Nanocrystals of
lovastatin was prepared by using simple precipitation method to overcome the difficulty of poor solubility and with less concentration of drug with proper selection of solvent and at proper dilution of drug solution with water, nanocrystals of lesser particle size is possible with slight change in crystallinity. The nanocrystals of lovastatin showed the enhanced saturation solubility, increased dissolution rate and more bioavailability in biological fluid.
Abstract:
Intranasal (IN) administration of drug continues to receive attention as an alternative route to systemic drug delivery due to its noninvasiveness. The benefits offered by nasal mucosa include large surface area, rapid drug onset, potential for CNS delivery, and no first-pass metabolism. A wide variety of therapeutic compounds can be delivered intranasally, such as antibiotics, vaccines, DNA and also relatively large molecules such as peptides and proteins, particularly in the presence of permeation enhancers. The nasal mucosa presents an ideal site for mucoadhesive drug delivery systems. Mucoadhesion is a good strategy to improve the systemic drug delivery via nasal route. Absorption rate and plasma concentration achieved after drugs delivered by intranasal route are comparable with that obtained by intravenous administration. The current review projects towards the different dosage forms for nasal delivery, physicochemical properties of drug and formulation & physiological factors affecting nasal delivery. The article also highlights mechanism of mucoadhesion and factors affecting the same.
Abstract: Recently, controlled and sustained drug delivery have become the standard in modern pharmaceutical world and an intensive research has been undertaken in achieving much better drug product effectiveness, reliability and safety. Hydrogel based devices belong to the group of swelling controlled drug delivery systems. Over the past few decades, advances in hydrogel technologies have spurred development in many pharmaceutical applications including controlled drug delivery. Many novel Hydrogel based delivery matrices have been designed and fabricated to fulfill the ever-increasing needs of the pharmaceutical and medical fields. This article reviews general introduction of hydrogel, drug release mechanism from hydrogel, polymers used in hydrogels, stimuli sensitivity of hydrogel & lastly applications of hydrogels to pharmaceutical field.
Abstract: ABSTRACT
The eye presents unique opportunities and challenges when it comes to the delivery of pharmaceuticals. While absorption by this route is bungling, there are few side effects with conventional ocular dosage forms. Hence, Ocular Polymeric Films are prepared to prolong the release of drug within the eye cavity. Moxifloxacin is a 4th generation fluoroquinolone useful in the treatment of eye infection such as conjunctivitis, keratitis and keratoconjuctivitis.
In this research work, four different formulations of mucoadhesive ocular films were prepared by using moxifloxacin as a model drug; and Hydroxy Propyl Methyl Cellulose (HPMC), Methyl Cellulose (MC), Sodium alginate and Poly Vinyl Alcohol (PVA) as polymers. The polymeric films were prepared by solvent casting method and PEG-400 was incorporated as plasticizer. The prepared ophthalmic films were then evaluated for uniformity of thickness, weight, drug content, % moisture absorption, % moisture loss and folding endurance. In vitro drug release of film was performed by studying the diffusion through artificial prehydrated cellophane membrane.
By considering all physicochemical parameters and in vitro drug release studies, the formulation MF4 with PVA (7%) was found to be best among all four formulations. So MF4 is selected as most promising and optimized formulation of moxifloxacin ocular film.
Abstract: Gatifloxacin ocular inserts were prepared by solvent casting method using different polymers in different ratios using PEG and glycerin as plasticizers. The physico-chemical parameters of the ocular inserts were evaluated. The stability of the drug in the formulations were confirmed by IR studies. In-vitro diffusion studies in phophate buffer pH 7.4 through artificial membrane (prehydrated cellophane membrane) and mechanism of drug release are identified. The ocular inserts containing Drug:HPMC (1:4:5) and Drug MC (2:9) showed best release with 93.15% and 90.53% at the end of 12 and 10 hours respectively. Among the different formulations, the best formulation was Drug:HPMC (1:4:5) since it showed retarded release of drug up to 12 hours. The formulations of Sodium CMC showed slightly faster drug release when compared to HPMC and MC films. The formulation prepared using gelatin filma could not sustain the drug within 2-3 hours. The gelatin films could not sustain the drug release. The data demonstrated that controlled release ocular inserts of gatifloxacin can be developed using HPMC in the ration of 1:4:5.
Abstract: Solventless compression coating was one of the strategies for delivering drugs to the colon after a period of lag time based on gastrointestinal pH and transit time concept. The present study was aimed to develop rapidly disintegrating core tablets containing indomethacin prepared by direct compression technique and compression coated with a mixture of naturally occurring time dependent hydrophilic swellable polymer hydropropylmethylcellulose (HPMC) and pH dependent or responsive soluble polymer eudragid S 100 (ED) in different percentage ratios. The effect of proportion of HPMC-ED coat mixture on lag time or premature drug release in upper part (stomach and small intestine) of gastrointestinal tract and amount of drug release in target area colon was studied. All the formulation showed a lag time of 3-5h depending upon proportion of HPMC-ED mixture in the coat. The formulation containing 60% HPMC and 40% of ED found to be suitable for targeting drugs like indomethacin to the colon which shows a lag time of 5h and releases 97% of drug in the target area. The presence of Eudragit in hydrophilic compression coat retarded the swelling of the coat in acidic to weakly acidic pH, but in alkaline pH, enhancement in drug release rate was observed due to the dissolution of Eudragit from the coat with time resulting in a porous coat structure, resulted in a faster and controlled drug release around 90–97% release in the target area.
Abstract: Intranasal administration is an ideal alternative to the parenteral route for
systemic drug delivery. Various conventional dosage forms have been employed for
this purpose but they lack to provide the desired bioavailability of the drug due to
poor residence time and faster clearance in the nasal cavity. Formulating
multiparticulate system with mucoadhesive polymers may provide a significant
increase in the nasal residence time. Neostigmine bromide, a cholinesterase inhibitor
is conventionally given by oral and i.v. route for the treatment of myasthenia gravis.
The aim of the present approach was to overcome the drawbacks of the conventional
dosage forms by formulating intranasal microspheres of Neostigmine Bromide with
Carbopol 974P NF and HPMC K15 M along with film forming polymer ethyl
cellulose by emulsion-solvent evaporation method. The prepared microspheres were
characterized for encapsulation efficiency, drug loading, particle size, surface
morphology, degree of swelling, in-vitro mucoadhesion, drug release, in-vivo studies
and stability studies. Formulations IN1 and IN5 displayed the best results for carbopol
and HPMC based microspheres respectively. Entrapment efficiency was 75.74±0.50
and 70.27±0.61; mucoadhesion was 98.5 and 85.3; and drug release up to 8 h was
87.86 and 84.5 for IN1 and IN5 respectively. In-vitro studies conclude that carbopol
based microspheres are better than HPMC based microspheres for the delivery of
neostigmine Bromide. Stability studies indicated that the formulations were most
stable at 4°C. In-vivo studies revealed that the formulations IN1 and IN5 showed
good bioavailability compared to oral drug administration.
Abstract: The present study aimed at preparing a novel time dependent pulsed release
system containing ‘Tablet-in-Capsule’ for the programmed release of salbutamol
sulphate for the treatment of nocturnal asthma. The core tablets of salbutamol
sulphate were prepared using wet granulation containing a superdisintegrant. Physical
characterization of tablet and powder blends used to form the core tablet was under
taken using a range of experimental technique. Eudragit S100 and Eudragit L100
were used as pH dependent polymers for coating the core tablet which were filled in
to the capsule. The ratio of Eudragit S100 and Eudragit L100 and the coating level
was optimized using 32 full factorial designs. Factors studied in design were
percentage of Eudragit S100 in combination with Eudragit L100 and the effect of
coating level on In-vitro drug release. Dissolution studies of ‘Tablet-in-Capsule’
device in media with different pH (1.2, 5.5, 6.8 and 7.4) showed that drug release in
colon could be modulated by optimizing the concentration of Eudragit L100: Eudragit
S100 (1:2). The study showed that, lag time prior to drug release was highly affected
by the coating level. The dissolution data reveled that the level of coating and the ratio
of polymers are very important to achieve a optimum formulation. The In-vitro
release from optimized formulation was found to be independent of paddle speed. The
gamma scintigraphic study pointed out the capability of the system to release drug in
lower parts of GIT after a programmed lag time for nocturnal asthma. Stability study
of the optimized formulation indicates no significant difference in release profile after
a period of one month.
Abstract: The field of Ocular drug delivery is one of the interesting and challenging
endeavors facing the pharmaceutical scientist. The most frequently used dosage forms
i.e. ophthalmic solutions and suspensions are compromised in their effectiveness by
several limitations, leading poor ocular bioavailability. In situ hydrogels are instilled
as drops into the eye and undergoes a sol to gel transition in the cul-de-sac, improved
ocular bioavailability by increasing the duration of contact with corneal tissue,
thereby reducing the frequency of administration. The purpose of the present work
was to develop an ophthalmic drug delivery system using the three different gelling
agents with different mechanisms for in situ gelation of Moxifloxacin hydrochloride,
a fluoroquinolone antibiotic. Polyox – a pH sensitive gelling agent, sodium alginate –
an ion sensitive gelling agent and Poloxamer – a temperature sensitive gelling agent
were employed for the formation of in situ hydrogel along with HPMC K4M as
viscofying agent. The promising formulations MF4, MF5 and MF9 were evaluated for
pH, drug content, in vitro gelation, in vitro drug release, in vivo drug release, ocular
irritation, and stability. Percent drug content of 98.2%, 98.76% and 99.43%; viscosity
of 15.724×100 cP, 16.108×100cP and 15.213 ×100 cP at 20 rpm, cumulative percent
release of 75.364%, 74.081% and 71.752%, and Cmax of 1164.16, 1187.09 and
1220.58 ng/ml was observed for formulation MF4, MF5 and MF9 respectively. The
developed formulations were therapeutically efficacious, stable, non-irritant and
provided sustained release of the drug over an 8 hour.
Abstract: The present work was based on “DESIGN AND PHYSICO-CHEMICAL
CHARACTERIZATION OF TABLET CONTAINING NOVEL
ANTIDEPRESSANT DRUG USING VARIOUS FORMULATION
TECHNIQUESâ€. 32 full factorial experiment was designed to study the effect of
Concentration of HPMC (X1) and PEO (X2) combination on the % cumulative
release after two hours (Y1), after 6 hours (Y2) and on the % cumulative release after
10 hours (Y3) in the core tablet. In vitro release profiles of all the batches were
performed with the kinetic model studies. Response surface graph were presented to
examine the effects of independent variables on the responses studied. The optimized
factorial batch was further given the functional coating to control the release. 32 x 21
factorial design was applied to study the effect of ratio of polymer:plasticizer (X1), %
coating (X2) and grade of polymer(X3). Polymer grade was used at 2 levels, whereas
other two factors at 3 levels. The final optimized batch was kept for 3 months of
stability study according to ICH guidelines and formulation was found to be stable
after 3 months of study. The optimized batch was studied for the dissolution kinetic
modeling.
Abstract: The skin can be used as the site for drug administration for continuous transdermal
drug infusion into the systemic circulation. For the continuous diffusion/penetration
of the drugs through the intact skin surface membrane-moderated systems, matrix
dispersion type systems, adhesive diffusion controlled systems and micro reservoir
systems have been developed. Various penetration enhancers are used for the drug
diffusion through skin. In matrix dispersion type systems, the drug is dispersed in the
solvent along with the polymers and solvent allowed to evaporate forming a
homogeneous drug-polymer matrix.
Matrix type systems were developed in the present study. In the present work, an
attempt has been made to develop a matrix-type transdermal therapeutic system
comprising of Ondansetron-HCl with different ratios of hydrophilic and hydrophobic
polymeric combinations using solvent evaporation technique. The physicochemical
compatibility of the drug and the polymers was studied by infrared spectroscopy. The
results obtained showed no physical-chemical incompatibility between the drug and
the polymers. The patches were further subjected to various physical evaluations
along with the in-vitro permeation studies using rat skin. On the basis of results
obtained form the in-vitro study and physical evaluation the patches containing
hydrophilic polymers i.e. polyvinyl alcohol and poly vinyl pyrrolidone, with oleic
acid as the penetration enhancer(5%) were considered as suitable for large scale
manufacturing with a backing layer and a suitable adhesive membrane.
Abstract: Background and objective: Solid lipid microparticulate (SLM) represents an alternative carrier system to traditional carrier colloidal carrier such as emulsion, liposomes and polymeric micro and nano particles. SLM combine the advantages of the traditional system such as emulsion, but avoid some of its major disadvantage such as instability and short self life.
Methods: The solid lipid microparticulate prepared by Hot homogenization method was found to be least particle size. Typically SLM were composed of lipid (Glyceryl mono stearate), surfactant (sodium taurocholate), acetone, ethanol and water. Factors such as rate of stirring, rate of homogenization, stirring time and speed were standardized to reduce the particle size.
Results: Particle size was characterized by using optical microscope and found to be 21.40 mm. The SLM were studied for its in vitro release characteristics by HPLC and found that 90.3 % of drug has been released from final formulation in 90 mins. While marketed product sirolimus tablet showed 65.5 % release in 90 mins. Entrapment efficiency of SLMs showed 98.02% while assay of marketed product was 98.6%. Different techniques like IR and SEM were used for the characterizations of SLMs. Finally, Sirolimus SLMs was incorporated into the soft gelatin capsule and comparatively evaluated with the marketed sirolimus tablet.
Interpretation and conclusion: It has been concluded that Hot homogenization method can be successively adopted for preparation of solid lipid microparticulate of Sirolimus. The lipid microparticulates were evaluated and found to immediate release of sirolimus and compared to market sirolimus tablet which also has immediate release profile of sirolimus. Thus, formulation of solid lipid microparticulate has been easily prepared with adequate physical properties and release properties advantageous for oral delivery of sirolimus and improves oral bioavailability.
Abstract: The benefits of intravenous infusion closely duplicated, without its hazards by using the skin as the port of drug administration to provide continuous transdermal drug infusion into the systemic circulation. To provide continuous drug infusion through the intact skin, membrane-moderated systems, adhesive diffusion controlled systems, matrix dispersion type systems and micro reservoir systems have been developed for the topical application on to the intact skin surface to control the delivery of drug and its subsequent permeation through the skin tissue. In matrix dispersion type approach, the drug reservoir is formed by homogeneously dispersing the drug solids in a hydrophilic or lipophillic polymer matrix and the medicated polymer is then molded into medicated disc with a defined surface area and controlled thickness. Matrix type systems were developed in this investigation, as they are easy to fabricate in a wide range of sizes and shapes and free from dose dumping in case of rupture.
The purpose of this research work was to develop a matrix –type transdermal therapeutic system containing diltiazem Hcl with different ratios of hydrophilic and hydrophobic polymeric combinations by the solvent evaporation technique. The physicochemical compatibility of the drug and the polymers was studied by infrared spectroscopy. The results suggested no physical chemical incompatibility between the drug and the polymers. The formulations were subjected to various physicochemical studies, in vitro drug permeation studies and ex- vivo permeation studies using human cadaver skin. The results followed the Higuchi kinetics (r = 0.997-0.999), and the mechanism of release was diffusion mediated. Based on physicochemical and ex-vivo permeation studies, patches coded as D3 (ethyl cellulose: polyvinylpyrrolidine7.5:2.5) and D6 (Eudragit RL 100: Ethyl cellulose 8:2) were chosen for further stability studies. The results indicate that the selected formulations were stable. In conclusion, the drug loaded polymeric films composed of D3 [EC: PVP (7.5:2.5)] and D6 [ERL 100: EC (8:2)] with 5% Tween 20 as permeation enhancer should be selected for manufacturing transdermal patch by using a suitable adhesive layer and backing membrane . Further in vivo performance studies are required.
Abstract: The particulate form of albumin has been regarded as a potential carrier for parenteral controlled drug delivery systems. In the present study, albumin microspheres of antihypertensive drug hydralazine hydrochloride were prepared by emulsion cross-linking method by using glutaraldehyde as cross-linking agent. Hydralazine hydrochloride, a vasodilator with short half-life and significant first-pass metabolism was taken as the model drug. To determine the effect of polymer concentration and amount of glutaraldehyde, formulations were characterized for their entrapment efficiency, particle size, surface morphology and release behavior. Maximum percentage entrapment efficiency (%EE) was found to be 68.20±1.03 %. Laser particle size analyzer confirmed mean particle size in the range of 31.7 to 39.6μm. The results showed that as increase in polymer concentration, there was significant increase in %EE and particle size. Scanning electron microscopy of microspheres revealed a spherical with smooth surface particles. In vitro drug release studies showed a biphasic release pattern for all formulations with an initial burst effect followed by slow release for almost 24 hrs. As comparing various kinetic models, different batches showed Fickian and diffusion mechanism for drug release. The release behavior was significantly regulated by polymer concentration and volume of glutaraldehyde. In vivo study to determine antihypertensive effect of selected formulation strongly correlating with in vitro drug release behavior of that particular formulation. The study revealed that hydralazine hydrochloride loaded albumin microspheres exhibited prolonged reduction of systolic and diastolic arterial pressure compared to hydralazine hydrochloride solution.
Abstract:
The present study was designed to evaluate targeting efficiency of carboplatin anticancer drug. Drug was encapsulated in natural biodegradable polymer (sodium alginate).The nanoparticles were prepared by the ion jellification technique and evaluated for encapsulation efficiency, zeta potential, loading capacity, in-vitro release pattern and targeting efficiency. Drug encapsulation efficiency was about 52.24 % to 61.70 % for different formulations. In vitro release profile shows that duration of drug release was also increased (more than 12 hrs) by nanoparticulate formulation as compared to pure drug (upto 3 hrs only. The formulations was parentally administered to mice and the drug was detected in body organs (liver, lungs and spleen) in case of free drug less amount of drug were found in liver, lungs and spleen as compared to drug encapsulated nanoparticles. Thus sodium alginate nanoparticles can be used for targeting carboplatin and it can be a promising tool in the delivery of anticancer drugs.
Abstract: A major hurdle in pharmaceutical formulation is water insolubility of most of the drugs affecting stability and bioavailability of the drug, if the drug is also insoluble in organic medium, it is difficult to deliver the drug in a sufficiently bioavailable form and hence it is a great challenge to formulation researchers to overcome such difficulty. Although some approaches are available for enhancing the dissolution of poorly soluble drugs but has certain draw backs like use of organic solvents, low drug loading and large doses. However, a new solution to poorly water soluble drug candidates is now available i.e. nanonisation and it leads to much more soluble, more biologically available and safer dosage form of poorly soluble and poorly bioavailable drugs.
In the present work, a nanocrystal of lovastatin was formulated by using simple precipitation method to overcome the difficulty of poor solubility and it was found that formulation with less concentration of drug with proper selection of solvent and at proper dilution of drug solution with water, nanocrystals with less particle size is possible with slight change in crystallinity. It has shown that, the drug has enhanced saturation solubility, increased dissolution rate and more bioavailable in biological fluid.
Abstract: Drug companies spend more than $5 billion per year on IT. So what does this
mean for drug delivery and formulation development as we know? An injectable
or solid oral immediate or sustained released are “no brainers†for pharma in terms of
dosage form selection. Now go have fun with solubility and stability, and its headache
time or cocktail time, depending where you are in the world and your choice of vice.
To combine the right chemical ingredients in the right proportions, driving the right
reactions under the right conditions to achieve the right end product with the right
properties requires an incredible amount of information and an incredible amount
of knowledge. All this information and knowledge has to be available at the point
of formulation. Managing the formulation process without iteration is the secret
to reducing development time. Having software to provide the right information
at the right place at the right time and you avoid costly, embarrassing mistakes
and eliminate duplicate work. Today, a formulator could even identify promising
formulation leads, store, and manage a pharma company’s formulation portfolio or
library. To quickly discard all about the leading options and eliminating time wasted
on low probability routes while identifying the best and least expensive ingredient
mix can save money and time. In the final analysis, this will allow drug delivery
companies to be in a greater position of strength. Drug delivery companies can
improve their odds of solidifying licensing and development deals on better terms.
Abstract: The invention relates to aquasome formulations for effective treatment of cancer. It specifically relates to site specific drug delivery formulations in the form of aquasome for administration of anticancer agent. More specifically it relates to site specific drug delivery formulations for administration of etoposide nanoparticles in the form of aquasome and process for preparation of such aquasomes. Etoposide immobilized onto hydroxyapetite core to form aquasome to reduce the toxicity and need for large doses. Etoposide loaded aquasomes were prepared by lyophilization method and were characterized for their particle size, surface morphology, zeta potential, encapsulation efficiency, in-vitro drug release, in-vivo tissue distribution studies, in-vivo pharmacokinetic studies and stability studies. All the nanoparticles found to be smooth and spherical shape. Particles size of the drug loaded nanoparticles revealed that the particles were found in nanometer range. The in vivo drug targeting studies revealed that, the drug loaded nanoparticles showed preferential drug targeting to lungs followed by liver, kidney and spleen. It was also revealed that, as compared to pure drug, higher concentration of drug was targeted to the organs like lungs and liver after administering the dose in the form of nanoparticles.
Abstract: The invention relates to ethosome compositions for transdermal drug delivery. It specifically relates to transdermal drug delivery compositions in the form of elhosomes of curcumin. More specifically, it relates to transdermal drug delivery ethosome compositions of curcumin in the form of ge] and process lor preparation of elhosomes and their gel forms. The present approach is to overcome the drawbacks of the conventional dosage forms by formulating elhosomes of curcumin using phospholipon 90H, cholesterol ethanol, propylene glycol, distilled water by cold method. The prepared ethosomes were characterized for their entrapment efficiency percentage. Particle Size and size distribution, Zeta Potential, Vesicle Morphology, Degree of Deformability. compatibility study by IR Spectroscopy and DSC, and XRD. The prepared ethosomal gel and free drug gel were characterized for their pH. Spreadability. Consistency, Homogeneity, in vitro drug release behavior, drug deposition study, in vivo studies, and Short term stability study. In vitro studies conclude that ethosomal gel is better than free drug gel for the delivery of curcumin. In vivo studies revealed that the formulation G-5 (ethosomal gel) showed good bioavailability compared to G-6 (free drug gel).
Number of Pages = 30
Abstract: The invention relates to proliposomal formulations for effective treatment of cancer. It specifically relates to site specific drug delivery formulations in the form of proliposomes for administration of anticancer agent. More specifically it relates to site specific drug delivery formulations for administration of PacJitaxel in the form of proliposome and process for preparation of such proliposomes. The formulations were prepared by modified film hydration method using EPG, DSPC in ratio of 1:4 to 1:10 and evaluated for Particle size, Zeta potential, Entrapment efficiency, in vitro drug release, in vivo bioavailability studies. The DSC studies revealed the absence of melting peaks of PTX in DSC thermograms of proliposomes formulations. This indicated that the drug may be dispersed in the form of amorphous state and which is confirmed with XRD studies. The stability studies indicated that the proliposomes prepared are stable.
Abstract: The present invention relates to novel di-aryl substituted imidazo [2,1-b] benzothiazole compounds, their stereoisomers, tautomeric forms, their regioisomers, polymorphs, esters, metabolites, and prodrugs, their pharmaceutically acceptable salts and their pharmaceutically acceptable solvates to compositions of any of the aforementioned embodiments together with pharmaceutically acceptable carriers, and to uses of any of the aforementioned embodiments as analgesic, anti-inflammatory, anticancer, antibacterial and antifungal activities. More particularly, the present invention relates to di-aryl substituted imidazo [2,1-b] benzothiozole derivatives and process for their preparation. We have synthesized a series of substituted diaryIimidazo-[2,l-b]-benzothiazole derivatives by reacting 2-amino benzothiazole with an appropriately substituted α-bromo-l,2-(p-substituted) diaryl-1-ethanones. The derivatives were characterized by spectral studies using IR, 1H NMR, 13C NMR, MS and HRMS. All the synthesized compounds were evaluated biologically for their analgesic, antiinflammatory, anti-tumour, antibacterial and antifungal activities.
Abstract: The present invention relates to a novel time dependent pulsed release system containing "Tablet-in-Capsule" for the programmed release of salbutamol sulphate for the treatment of nocturnal asthma. The core tablets of salbutamol sulphate were prepared using wet granulation containing a superdisintegrant. Physical characterization of tablet and powder blends used to form the core tablet was under taken using a range of experimental technique. Eudragit S100 and Eudragit LI 00 were used as pH dependent polymers for coating the core tablet which were filled in to the capsule. The ratio of Eudragit S100 and Eudragit L100 and the coating level was optimized using 32 full factorial designs. Factors studied in design were percentage of Eudragit SI 00 in combination with Eudragit LI 00 and the effect of coating level on In-vitro drug release. Dissolution studies of"Tablet-in-Capsulc" device in media with different pH (1.2, 5.5, 6.8 and 7.4) showed that drug release in colon could be modulated by optimizing the concentration of Eudragit L100: Eudragit S100 (1:2). The study showed that. tag time prior to drug release was highly affected by the coating level. The dissolution data revealed that the level of coating and the ratio of polymers are very important to achieve a optimum formulation. The In-vitro release from optimized formulation was found to be independent of paddle speed. The gamma scintigraphic study pointed out the capability of the system to release drug in lower parts of GIT after a programmed lag time for nocturnal asthma. Stability study of the optimized formulation indicates no significant difference in release profile after a period of one month.
Abstract: The present invention relates to multi purpose herbal compositions for treatment of various diseases such as Liver diseases. Diabetes, Arthritis, Inflammation etc. The herbal composition particularly comprises an effective amount of an extract and/or at least one bioactive fraction or powder from herbs such as Annona squamosa and Nigella sativa; and process for the preparation of such extracts and herbal compositions. The results showed that Herbal composition have significant Hepatoprotective, Antilipidemic, Antiarthritic, antiinflammatory and Analgesic properties. In CCl4 induced liver fibrosis in male Wister albino rat"s model combination of both herbs significantly decreased CCl4 induced elevation of serum transaminase activities, hyaluronic acid, laminin and procollagen type III levels, and contents of hydroxyproline in liver tissue by approximately 30-60%. When treated with 100 and 150 mg/kg, ig. It also restored the decrease in SOD and GSH-Px activites and inhibited the formation of lipid peroxidative products during CCl4 treatment. In another study combination of extract (PHF) administered orally (200 mg/kg body weight) for 30 days showed significant reduction of blood glucose and increase in plasma insulin. Herbal composition also resulted in a significant decrease in tissue lipids and lipid peroxide formation. In another study Herbal composition reduced hind paw swelling, body weight, AST, ALT and TP Histopathology revealed significant reduction in mononuclear infiltration, pannus formation and bone erosion when arthritis was induced by Complete Freund"s Adjuvant (CFA) injection in metatarsal footpad of Sprague-Dawley rats. Herbal composition also shows moderate central and peripheral analgesic activities in hot plate method and acetic acid induced writhing method in mice.
Abstract: The present invention relates to herbal compositions for treatment of Inflammation and Arthritis. The herbal composition particularly comprises an effective amount of an extract and/or at least one bioactive fraction or powder from one or more medicinal herbs such as Sesbania grandiflora, Sesbania sesban and Terminalia chebula; and process for the preparation of such extracts and herbal compositions. In carrageenan induced model, the extracts of Sesbania grandiflora, Sesbania sesban and Terminalia chebula were able to significantly reduce paw edema. This anti edematous effect was significant during the first phase of inflammation indicating the inhibition of histamine release. It was found that the petroleum ether extracts of bark of Sesbania grandiflora and Sesbania sesban; and fruit of Terminalia chebula as well as various compositions of A, B, C and D exhibited anti-arthritic effect evidenced by increase in body weight, R.B.C., Hb and thymus weight and decreased edema formation, WBC level, ESR level and reduce swelling occurs at spleen sites and in comparison with arthritic control animals. The results suggest that petroleum ether extracts of bark of Sesbania grandiflora, Sesbania sesban and fruit of Terminalia chebula showing better anti-inflammatory activity than other chloroform and methanol extracts of S. grandiflora, S. sesban and T chebula. However, due to their better anti-inflammatory activity same extracts were utilized and on the basis of these potent effects of individual herbal plant extracts, the different synergistic compositions like A, B, C and D were prepared and which show considerable potency in anti-inflammatory action and has prominent effects on adjuvant arthritis by alleviating paw edema.
Abstract: The present invention is directed to a pharmaceutical composition for enhancing the oral bioavailability of a prodrug ester by formulating the ester as a non-aqueous formulation with medicum chain triglycerides (MCTs). It particularly relates to a ester prodrug as a non-aqueous formulation. Non-aqueous formulations include solids, tablets, capsules, lozenges, suspensions, elixirs and solutions. A suitable prodrug ester is a cephalosporin β-lactam antibiotic such as cefuroxime axetil in a non-aqueous suspension. Pharmaceutical compositions of a ester prodrug for enhancing the oral bioavailability comprising the effective amount of ester prodrug and medium chain triglycerides, the ester prodrug is selected from group consisting of antibiotics, corticosteroids, Non Steroidal anti-inflammatory drugs, Anti retroviral and Angiotensin II antagonists. The ester prodrug is selected from antibiotcs such as cefuroxime axetil, cefpodoxime proxetil or cefetamet pivoxil and preferably cefuroxime axetil in effective amount is 1 to 10 % (w/v). The medium chain triglycerides are derived from coconut oil and/or palm seed oil in an amount between 1 nd 50% (v/v). The composition is in the form of oral nonaqueous suspension. The composition further comprises one or more pharmaceutical excipient or carrier. A process for preparing pharmaceutical composition of a ester prodrug for enhancing the bioavailability comprising the step of mixing the ester prodrug with medium chain triglycerides. The ratio of cefuroxime axetil to medium chain triglycerides ranges from 1:1 up to 1:5. The bioanalytical method for the determination of Cefuroxime was fully validated
Abstract: The invention relates to controlled drug delivery formulations for parenteral administration of active agent. The controlled drug
delivery formulations in the form of microspheres are developed for parenteral administration of antihypertensive agent. The
controlled drug delivery formulations developed in the form of albumin microspheres for intramuscular administration of Hydralazine
HCl to give during emergency and to avoid complications associated via other routes and with a view of giving a prolonged release of
the Hydralazine HCl. Microspheres were prepared with natural polymer BSA using emulsion polymerization technique or emulsion
cross-linking method. The prepared microspheres proved to be a potential candidate for microparticulate parenteral controlled drug
delivery system.
Abstract: The invention relates to nanocrystals of poorly water soluble drugs to increase their solubility and dissolution rate and thereby
increased bioavailability. It specifically relates to the preparation of statin nanocrystals. More particularly it relates to the easy and
cost-effective process for preparation of lovastatin nanocrystals and its formulations for convenient oral delivery. Nanocrystals of
lovastatin was prepared by using simple precipitation method to overcome the difficulty of poor solubility and with less concentration
of drug with proper selection of solvent and at proper dilution of drug solution with water, nanocrystals of lesser particle size is
possible with slight change in crystallinity. The nanocrystals of lovastatin showed the enhanced saturation solubility, increased
dissolution rate and more bioavailability in biological fluid.
