Formulation Design and Evaluation of Ornidazole Microsphere in a Bioadhesive gel for Local Therapy of Vaginal Candidiasis

The aim of present work is to design a novel vaginal drug delivery system composed of Ornidazole microspheres incorporated in a bioadhesive gel. Microspheres were prepared by solvent evaporation method by using Eudragit RS 100 and Eudragit RL 100 polymers with different drug/ polymer ratios. The microspheres were found to be discrete, spherical with free flowing properties and evaluated for particle size analysis, shape (SEM), drug entrapment efficiency, percentage drug loading, and in vivo drug release studies. The selected microsphere formulation (F7 and F8, containing drug polymer ratios 1:1:1 and 1:0.25:1.75 respectively) was incorporated in a bioadhesive carbopol 934P gel. The formulation (F8.ODZ-MG) which showed maximum of 91.03% release at 8h was then subjected to stability studies and antifungal activity. The antifungal activity of the F8.ODZ-MG and placebo gel was evaluated against Candida albicans 1012 by using cup plate method. This showed that ODZ-MG was capable to control the growth of Candida albicans for more than 14h. Placebo gel did not show any zone of inhibition. Stability studies were done as per ICH guidelines for a period of 6 months. Initial and third month studies were done and evaluated for parameters such as pH, drug content, drug content uniformity, extrudability, spreadability, viscosity and in vitro drug release. The results showed that there were no significant changes in the drug content and in vitro drug release. It may be concluded from the present study that ODZ-MG can be used as a novel delivery system for local therapy of vaginal candidiasis.