Enhanced transdermal delivery of an anti HIV agent via ethanolic liposomes

Indinavir, a protease inhibitor depicts short biological half life, variable pH dependent oral absorption with extensive first pass metabolism thus presenting a challenge concerning its oral administration. The current work aims to formulate and characterize indinavir bearing ethanolic liposomes (ethosomes), and investigate their enhanced transdermal delivery potential. The prepared ethanolic liposomes were characterized to be spherical, unilamellar structures having low polydispersity (0.12±0.03), nanometric size range (147 ± 4.5 nm) and better entrapment efficiency (96.71±1.4%). Permeation studies of indinavir across human cadaver skin depicted enhanced transdermal flux of 27.2±4.2 µg/cm2/h from ethanolic liposomes which was significantly (P<0.05) greater than ethanolic drug solution (13.2±2.7 µg/cm2/h), conventional liposomes (6.3±1.5 µg/cm2/h) and plain drug solution (3.2±1.2 µg/cm2/h), respectively. Additionally, the ethanolic liposomes depicted shortest lag time (0.41 h) for indinavir, thus presenting a suitable approach for transdermal delivery of this protease inhibitor.