Lamivudine Liposomes for Transdermal Delivery - Formulation, Characterization, Stability and In vitro Evaluation

Lamivudine, an antiretroviral is commonly used in the treatment of HIV infections. Upon oral administration, it exhibits dose dependent toxic effects such as hepatotoxicity, hyperglycemia, hyperlipidemia, lactic acidosis, lipodystropy, osteonecrosis. These side effects often require dosage reduction or even cessation of treatment. Thus, the problems associated with oral administration led us to explore the possibilities of designing novel drug delivery system for lamivudine with an alternative route of administration. In the present study, liposomes of lamivudine were prepared by thin film hydration and their potential for transdermal drug delivery has been evaluated in vitro. In the preparation of liposomes, process and formulation parameters were standardized. Liposomes were evaluated for their physicochemical properties such as appearance, particle size, particle size distribution and drug entrapment. Liposomes stored at lower temperature conditions, retained 96 % of the incorporated drug. Residual solvents in the formulation were determined by Gas Chromatography and content of lipids was estimated by Stewart assay. Permeation studies of liposomal formulations were carried out across rat abdominal skin using modified Franz diffusion cells. The lamivudine liposomes with good stability and appreciably controlled skin permeation with minimal retention of drug in the skin were successfully prepared.