Permeation Enhancer

The aim of present investigation was to develop nanoemulsion gel of ketoconazole for topical delivery and comparison with the marketed preparation. Ketoconazole, BCS class II antifungal agent with broad spectrum activity is a poorly soluble and highly permeable drug. Due to its poor solubility, it is incompletely absorbed after oral dosing and bioavailability varies. The drug efficacy of topical formulation can be limited by instability due to its poor solubility in the vehicle and low permeability. Therefore, to overcome these shortcomings of conventional system nanoemulsion have been used as drug carrier in topical treatment of fungal infection, especially in dermatology. Pseudo-ternary phase diagram was constructed on triplot software to identify nanoemulsion area using different concentrations of oil, Smix (surfactant and co- surfactant) and water. 2% Carbopol 980 as gelling agent and 0.5% DMSO as permeation enhancer was used in topical gel formulation. The formulations was characterized on the basis of pH, drug content, viscosity and in-vitro diffusion study. The optimized formulation was found to have pH 7.4 and drug content 98.90%. In-vitro diffusion study of nanoemulsion gel showed 80.375% release within 8 hrs. Drug release of ketoconazole nanoemulsion gel when compared with marketed formulation showed 80.375% release within 8 hrs as compare to 52.125% for marketed preparation (Ketoconazole cream 2%, H&H Pharmaceutical). So, it is concluded that by incorporating ketoconazole nanoemulsion in topical gel provided sustained release along with improved solubility and permeability.