| Topical Econazole Nitrate, an antifungal agent, is actively being investigated for the treatment of anti-fungal infections. This study was undertaken to develop and screen various topical formulations with optimum drug release and permeation through the skin.;Various formulations containing 0.50% and 0.25% drug were developed using cationic, non-ionic, cationic emulsion-based systems' along with HPMC gels. Also, the effects of penetration enhancers, Polyethylene Glycol, Dimethyl sulfoxide (DMSO) and Diethylene glycol monoethyl ether (DGME) at 5%, 10% and 15% levels were evaluated. In-vitro studies were performed with Franz Diffusion Cells using cellulose membrane and Human cadaver skin as the diffusion barriers for 2 hours. The samples with optimum drug release were further studied for a 12 hour period. The selected formulation with maximum drug release through cellulose membrane was then chosen for drug release through human cadaver skin.;With the cellulose membrane, the drug release order was observed to be HPMC gel base > non-ionic emulsion > cationic emulsion. The inclusion of additives at all levels had little or no effect in enhancing the drug release from these formulations. Among all samples tested, HPMC gel base with 15% DMSO gave 58.48% drug release in 2 hour and 72.45% after 12-hour period and next comparable formulation Non-ionic emulsion with 15% DMSO gave 38.97% after 2 hours and 59.46% after 12 hours. The drug release of these formulations was then studied through human cadaver skin for 12 hours. Here, the drug release pattern remained similar to cellulose membrane, but the amount of total drug diffused was reduced as expected. These data were treated to determine various physical parameters that influence drug diffusion. Interestingly, the values for the steady state flux and diffusion coefficient were found to be the highest from the optimum formulation, and the values for the lag time and partition coefficient were the lowest.;In vitro diffusion studies served well as a model to screen various dermatological formulations with optimum drug release profiles. The HPMC gel base containing 15% DMSO with 0.5% and 0.25% of Econazole Nitrate gave the optimum release of drug. This study supports that with a proper composition of a dermatological vehicle, it is possible to develop a topical formulation with optimal drug release for a better clinical effect. |
