title: Enhanced transdermal delivery of an anti-HIV agent via ethanolic liposomes.
abstract: Indinavir, as a protease inhibitor with a short biological half life, variable pH-dependent oral absorption, and extensive first-pass metabolism, presents a challenge with respect to its oral administration. The current work aims to formulate and characterize indinavir-bearing ethanolic liposomes (ethosomes), and to investigate their enhanced transdermal delivery potential. The prepared ethanolic liposomes were characterized to be spherical, unilamellar structures having low polydispersity, nanometric size range, and improved entrapment efficiency over other delivery formulations. Permeation studies of indinavir across human cadaver skin resulted in enhanced transdermal flux from ethanolic liposomes that was significantly (P < 0.05) greater than that with ethanolic drug solution, conventional liposomes, or plain drug solution. Additionally, the ethanolic liposomes showed the shortest lag time for indinavir, thus presenting a suitable approach for transdermal delivery of this protease inhibitor. From the clinical editor: This study characterizes indinavir bearing ethanolic liposomes (ethosomes), and investigate their enhanced transdermal delivery potential, demonstrating a potentially a suitable approach for transdermal delivery of this protease inhibitor for HIV treatment, which typically has been associated with limited bioavailability via the oral route.
authors.affiliation: Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, Dr. H.S. Gour University Sagar, India.
authors.forename: Vaibhav
authors.initials: V
authors.lastname: Dubey
authors.forename: Dinesh
authors.initials: D
authors.lastname: Mishra
authors.forename: Manoj
authors.initials: M
authors.lastname: Nahar
authors.forename: Vikas
authors.initials: V
authors.lastname: Jain
authors.forename: Narendra Kumar
authors.initials: NK
authors.lastname: Jain
mesh_terms: D000279:Administration, Cutaneous; D000431:Ethanol / Q000737:chemistry*; D017320:HIV Protease Inhibitors / Q000008:administration & dosage* / Q000737:chemistry / Q000494:pharmacology; D019469:Indinavir / Q000008:administration & dosage* / Q000494:pharmacology; D008081:Liposomes / Q000737:chemistry*; D046529:Microscopy, Electron, Transmission; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption
chemical_list: D017320:HIV Protease Inhibitors; D008081:Liposomes; D000431:Ethanol; D019469:Indinavir