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 glycerylmonostearate 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: 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: 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: 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: 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:
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.
