The rationale behind present work was to formulate a novel cream containing microsponges of miconazole nitrate to provide prolonged release. By means of quasi-emulsion solvent diffusion method using Eudragit RS-100 with different drug-polymer ratios microsponges were prepared. In the direction of optimizing microsponge formulation, diverse factors that affect microparticles physical properties were also investigated. Microsponges were characterized by SEM, DSC, FT-IR and particle size analysis, and also evaluated for morphology, drug loading and in vitro drug release. The drug polymer ratio reflected notable effect on drug content, encapsulation efficiency and particle size. It has been found that there was no chemical interaction between drug and polymers used as revealed by FT-IR and DSC spectra. SEM micrographs exposed that microsponges were spherical, with porous surface and have had 26.23 μm mean particle size. The microsponges were then incorporated in cream; which showed viscous modulus along with pseudoplastic behavior. In vitro drug release results depicted that microsponge with drug-polymer ratio of 1:2 was more efficient to give extended drug release of 78.28% at the end of 8 h; while conventional formulations get exhausted incredibly earlier by releasing 83.09% drug at the end of 4 h only. Thus the formulated cream containing microsponges of miconazole nitrate would be a promising alternative as compared to conventional therapy for secure and efficient treatment of acne and other topical infections.
Transdermal drug delivery system (TDDS) is not practicable for delivery of materials whose final target is skin itself. Controlled release of drugs onto the epidermis with assurance that the drug remains primarily localized and does not enter the systemic circulation in significant amounts is a challenging area of research. Microsponges are highly porous micro-sized particles with a unique ability for entrapping active pharmaceutical ingredients. To control the delivery rate of active agents to a predetermined site in human body has been one of the biggest challenges faced by scientists. Microsponges are safe biologically and offer unique advantage of programmable release. This technology offers entrapment of ingredients and is believed to contribute towards reduced side effects, improved stability, increased elegance and enhanced formulation flexibility. This technology is being used for topical formulations and also for oral administration. The present review describes microsponge technology including its preparation, characterization, programmable parameters and release mechanism of microsponge drug delivery system.
All drug delivery systems, oral drug delivery remain the most preferred option for administration for various drugs. Sustained Release is also providing promising way to decrease the side effect of drug by preventing the fluctuation of the therapeutic concentration of the drug in the body. The basic rationale of sustained drug delivery system optimizes of the biopharmaceutical, pharmacokinetic and pharmacodynamics properties of a drug in such a way that utility is maximized, side-effects are reduced and cure of the disease is achieved. Sustained release drug delivery is improved patient compliance due to less frequent drug administration, reduction of fluctuation in steady-state drug levels, maximum utilization of the drug, increased safety margin of potent drug, reduction in healthcare costs through improved therapy and shorter treatment period. The principal goal of sustained release forms is the improvement of drug therapy assessed by the relationship between advantages and disadvantages of the use of sustained release system.
Liquisolid technique is a new and promising method that can change the dissolution rate of water insoluble drugs. According to the new formulation method of liquisolid compacts, liquid medications such as solutions or suspensions of water insoluble drugs in suitable non-volatile liquid vehicles can be converted into acceptably flowing and compressible powders by blending with selected powder excipients. It has been speculated that such systems exhibit enhanced release profiles. In this case, even though the drug is in a solid dosage form, it is held within the powder substrate in solution or, in a solubilized, almost molecularly dispersed state, which contributes to the enhanced drug dissolution properties.
Objective: To explore a novel natural polymer, pullulan for controlling the release of fenoverine from matrix tablets and to elucidate the release kinetics of fenoverine from pullulan and HPMC matrices. Methods:In this study we formulated monolithic matrix tablets containing of fenoverine as controlled-release tablets by direct compression using pullulan, HPMC (Hydroxypropyl methyl cellulose) K4M and HPMC K100M polymers and evaluated for hardness, thickness, friability, weight variation drug content, in vitro drug release characteristics and FTIR (Fourier transform infrared spectroscopy) and DSC (Differential scanning calorimetry) study.Results: All the formulations showed compliance with pharmacopoeial standards. FTIR and DSC study indicated the absence of interaction between fenoverine and excipients. The formulation was optimized on the basis of acceptable tablet properties and in vitro drug release. The results of dissolution studies indicated that the formulation F5 [drug to polymer 1: 0.35] exhibited highest % cumulative drug release of 96.82±0.75 % at the end of 12 h. Optimised batch F5 showed super case II transport mechanism and followed zero order release kinetics. Short-term stability studies of the optimized formulation indicated that there were no significant changes observed in hardness, drug content and in vitro dissolution studies at the end of three months period. Similarity factor f2 was found to be 89, which indicated similar dissolution profiles before and after stability study. Conclusion:Based on above results we conclude that pullulan can be used as a polymer for retarding the release of drug from matrix formulations.
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