The objective of this study was to microencapsulate the anti-inflammatory drug (naproxen) to provide controlled release and minimizing or eliminating local side effect by avoiding the drug release in the upper gastrointestinal track. Naproxen was microencapsulated with lipid-like carnauba wax, hydrogenated castor oil using modified melt dispersion (modified congealable disperse phase encapsulation) technique. Effect of various formulation and process variables such as drug-lipid ratio, concentration of modifier, concentration of dispersant, stirring speed, stirring time, temperature of external phase, on evaluatory parameters such as size, entrapment efficiency, and in vitro release of naproxen were studied. The microspheres were characterized for particle size, scanning electron microscopy (SEM), FT-IR spectroscopy, drug entrapment efficiency, in vitro release studies, for in vitro release kinetics. The shape of microspheres was found to be spherical by SEM. The drug entrapment efficiency of various batches of microspheres was found to be ranging from 60 to 90 %w/w. In vitro drug release studies were carried out up to 24 h in pH 7.4 phosphate buffer showing 50-65% drug release. In vitro drug release from all the batches showed better fitting with the Korsmeyer-Peppas model, indicating the possible mechanism of drug release to be by diffusion and erosion of the lipid matrix.
Flavonoids are phytochemical compounds found in a variety of plants, fruits, vegetables, leaves, and barks, it offers a wide range of health benefits. Quercetin is a polyphenolic flavonoid that is found in onions, apples, berries, broccoli, grapes, nuts, cherries and many other food products. Pharmacologically, quercetin has been examined for various disorders and is reported to possess the ability to prevent as well as treat them. It possesses anti-oxidant, anti-allergic, anti-inflammatory, anti-viral and anti-cancer activity as well. Developing suitable formulation for the delivery of quercetin to specific site leads to better compliance and effective treatment of the disease. This review article highlights the beneficiary activities exhibited by quercetin along with the mechanism behind its activity, followed by reporting the different quercetin formulations developed in last few years.
Objective: Thermo-modulated in-situ hydrogel (TSHG) are formulated routinely utilizing poloxamer for extended drug release. However physical properties of such formulations may have some flaws, which can be rectified using a combination of polymers with better physical properties such as chitosan. The purpose of the present study was to fabricate biodegradable chitosan-poloxamer-based in-situ drug delivery systems and assessment of their physical properties. Methods: The present chitosan-poloxamer gel base was formulated using a two-stage method. Initially, chitosan gel was prepared by dissolving 1% w/w chitosan in glacial acetic acid. The poloxamer gel was prepared using “cold method”. The final chitosan-poloxamer gel base was prepared by mixing equal amounts of both solutions and evaluated for physical and mechanical properties. Result and Discussion: The DSC thermogram demonstrated no obvious interactions among ingredients or micellization temperature. The gelation temperature of the gel was between 27 and 330C. The pH was 7 with slight clarity. The viscosity of the gel ranged from 15.14 to 41.19 pa.s. The gel was syringable between 4-300C and biodegradable under physiological conditions. The mean particle size of the gel under SEM was found in the range of 300-554 nm. Conclusion: After the evaluation of the formulation, it can be concluded that all the ingredients in the gel showed good compatibility with each other, which could form a stable and homogeneous gel with favorable mechanical and physical properties. Keywords: chitosan, drug delivery system, hydrogels, poloxamer
Budesonide is a highly potent synthetic, nonhalogenated corticosteroid. The mechanism of action of corticosteroids in allergic rhinitis remains unknown, but may involve reductions in number of various mediator cells such as basophils, eosinophils, T-helper cells, mast cells, and neutrophils. In the nasal mucosa, nasal reactivity to allergens, and release of inflammatory mediators and proteolytic enzymes. Budesonide is very effective and quikly acting as it is rapidly and almost completely absorbed after oral administration, but has poor systemic availability (about 10%) due to extensive first-pass metabolism in the liver, mainly by the cytochrome P450 isoenzyme CYP3A4.. The major metabolites, 6-β- hydroxybudesonide and 16-α-hydroxyprednisolone have less than 1% of the glucocorticoid activity of unchanged drug with a terminal half-life of about 2 - 4 hours. Polymeric films containing Eudragit RL 100: Eudragit RS: drug (7:3:1, 7: 2:1) and Ethyl cellulose: PVP: drug (7:3:1, 7:2:1) were selected for transdermal administration based on evaluation studies. These polymeric films were prepared by mercury substrate method employing PEG-400 as plasticizer. Two different penetration enhancers Urea and Dimethyl sulphoxide (DMSO) were employed in the study. The patches in each group were uniform in drug content, thickness. In Vitro drug permeation, moisture absorption and WVTR studies were carried out on these test patches. It was found that at all humidity condition the absorption increases which were linear to the moisture absorbed. In PVA and EUDRAGIT RL 100 patches the water vapor transmission rate was found to be higher at 75% RH, RT conditions. Therefore at both % RH, RT condition the PVA and EUDRAGIT RL 100 patches provides the best resistance to water vapor. Therefore, when applied to animals (in further studies) these patches may provide more occlusion to water vapor loss from skin thus making atmosphere beneath the skin more humid that aid in drug permeation
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