Effect of various penetration enhancers on permeation kinetic of itraconazole for the topical drug delivery system

Abstract

Itraconazole (ITZ) is a synthetic triazole antifungal agent having topical and systemic efficacy against familiar fungi such as Aspergillus and other filamentous fungi. The difficulties of ITZ with oral administration like dissolution rate limited absorption and gastric side effects can be overcome by formulating it in topical system. The aim of the this study was to evaluate the effect of various penetration enhancers on permeation kinetic of ITZ using Franz diffusion cell through pretreated cellophane membrane for topical system. Various permeability parameters like steady state flux, permeability coefficient and enhancement ratio were calculated. The permeation rate of pure ITZ was found to be 33.27 µg/cm²/hr. All penetration enhancers (except cyclodextrin) showed 1 to 2 times enhancement ratio. The inclusion complex of the ITZ showed best drug permeation rate (452.20 µg/cm²/hr). It was concluded that ITZ inclusion complex with HPβCD is the best way of enhancing the permeation of drug through cellophane membrane for transdermal system.