IN-SITU GEL BASED MUCOSAL SITE-SPECIFIC DRUG DELIVERY SYSTEMS: FORMULATION AND EVALUATION

The aim of this study was to prepare a suitable mucoadhesive in-situ gel formulation of clotrimazole for the treatment of vaginal candidiasis. The in-situ gel-forming systems are viscous liquids that turn to a gel phase upon exposure to physiological conditions. The lower retention of conventional formulations in the vagina, mucoadhesive formulations would prolong the retention time.  For this study mixture of poloxamer (Plx) 407 and 188 were used. 3² full factorial design was applied for the optimization. Selected independent variables were concentration of carbopol 974 (X1), and Hydroxypropyl methylcellulose (HPMC) E50 (X2) was added to in situ gel for improve the mucoadhesive properties of the formulation, and prolong the residence time in vaginal cavity. Selected dependent variables were viscosity (Y1) release at 1 h (Y2), release at 12 h (Y3). After the preparation of mucoadhesive in-situ gels, gelation temperature/time, viscosity, mucoadhesive strength, spreadability, drug content, in-vitro drug release, and in-vitro antimicrobial efficacy were determined. Based on the obtained results and according to desirability, it was found that gel prepared with 20% Plx 407, 10% Plx 188, 1.5% HPMC (E50), and 1.5% carbolop 974 suitable for vaginal administration of clotrimazole.