Development and Characterization of Nanoemulgel Based Transdermal Delivery System for Enhancing Permeability of Tacrolimus

摘要

The purpose of this study was to develop and characterize the potential of transdermal nanoemulgel for enhancing solubility and dissolution rate of poorly water soluble drug Tacrolimus (TM). Pseudoternary phase diagrams were constructed using oleic acid as oil, cremophor RH 40 as surfactant, transcutol P as cosurfactant. The nanoemulsions were prepared by spontaneous emulsification method. The prepared nanoemulsions were subjected to different thermodynamic stability tests and characterized for cloud point measurement, precipitation studies, transmission electron microscopy, globule size, polydispersity index, viscosity, zeta potential, % transmittance conductivity and dye solubilization test. Almond gum was used as gel base to convert nanoemulsion into nanoemulgel. The optimized nanoemulgel (AF5) contained 20% oleic acid as oil, 65% cremophor RH 40 and transcutol P as surfactant co-surfactant mixture, 14% water and 1% w/w almond gum. Transdermal permeability of optimized nanoemulgel through rat abdominal skin was compared with the marketed formulation. Nanoemulgel showed significantly higher (P < 0.05) cumulative amount of drug permeated and flux, along with lower lag time and skin retention than marketed formulation. These results suggested that advanced permeation characteristics of nanoemulgel formulation may be an alternative compared to conventional formulations of TM for transdermal application.