Formulation and Evaluation of Ketoconazole Microsponge Topical Gel

Abstract

Microsponges are those drug delivery systems which are intended in a way to deliver a minimum dose of the drug or pharmaceutically active ingredient to increase the stability of formulation, to alter drug release profile. Ketoconazole is an imidazole anti-fungal agent belonging to BCS class II. The main objective of this research work is to formulate and evaluate ketoconazole microsponge for topical delivery by using various polymers such eudragit S-100, eudragit L-100 in four ratios 1:2, 1:3, 1:4, 1:5 by quasi emulsion method. The formulations prepared were labelled based on the ratios as ES 2. ES 3, ES 4, ES 5 for eudragit S-100 and EL 2, EL 3, EL 4, EL 5 for eudragit L-100. Evaluation tests like entrapment efficiency, production yield, drug content was performed and formulation of eudragit L-100 (EL 5) and eudragit S-100 (ES 5) showed better results. ES 5 and EL 5 formulations were optimized and tests like in vitro dissolution studies were conducted which showed that the formulation ES 5 showed released upto 8 hours and can be used in the formulation of gel. The gel (GES5) was prepared by usingmicrosponges containing the drug ketoconazole equivalent to 1 % w/w and was incorporated into the gel base made up of Carbopol 934. The microsponges were sieved and were dispersed in Carbopol gel. Evaluation tests like pH measurement, visual inspection, spreadability studies, drug content and in vitro diffusion studies. This method of formulating microsponges has improved drug delivery therefore helping in the enhancement of the bioavailability of the drug and also acts as an efficient carrier through the skin.