国际药物开发与研究杂志

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Formulation and Evaluation of Microsponges Loaded Topical Gel for Treatment of Acne Vulgaris

Diksha D Ghorpade1*, Dr. Atram SC2

The purpose of present study aims to design novel drug delivery system containing adapalene microsponges and to prepare microsponge gel. Adapalene is an anti-acne drug used in the treatment of acne infection having a poor aqueous solubility, side effects and adverse reactions. The microsponge delivery system is unique technology for controlled/ sustained release of active agents. The microsponges were prepared by quasi-emulsion solvent diffusion method by using polymer Eudragit S-100 and Eudragit RS -100. All the formulated microsponges were subjected for various evaluation parameters such as production yield, encapsulation efficiency, particle size analysis and in vitro drug release study. The optimized microsponge formulation F4 and F8 were further formulated as gel formulation for topical delivery. Prepared gel was evaluated for physical parameters like pH, spreadability, viscosity, drug content and in vitro diffusion study and compared with the other formulation. The Differential scanning calorimetry (DSC), XRD, Zeta potential and Particle size of drug and excipient confirm compatibility. Results revealed that quasi-emulsion solvent diffusion method is a suitable technique for the preparation of microsponges as most of the formulations were discrete and spherical in shape with a good production yield of 51.88 % to 89.41% and the highest drug release for MGF4 and MGF8 formulation was found to be 87.77 % and 83.24 % respectively for the 8 h. The drug release of microsponges gel is 91.31% .The drug release data of optimized batch MGI (F4) were fitted into different kinetic models and showed that the drug release from gel formulation follows zero order release. As compared to conventional formulation, the prepared microsponge gel is expected to remain on the skin for a longer time, gradually releasing their contents over the time. Hence, adapalene microsponges and microsponge gel prepared in this study are promising as being more useful than conventional formulation therapy.

Keywords

Adapalene; Microsponge; Anti acne drug; Microsponge gel; Topical delivery

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