Abstract

DESIGN AND DEVELOPMENT OF LIPOSOMES CONTAINING ARTESUNATE FOR THE TREATMENT OF P. FALCIPARUM MALARIA

Ramakrishna Shabaraya*, Ankit Santosh Parulkar, Krishnananda Kamath and Sripathy D.

ABSTRACT

NDDS is a system for delivery of drug other than conventional drug delivery system. NDDS is a combination of advance technique and new dosage forms which are far better than conventional dosage forms. Microparticles, microcapsules, nanoparticles, lipoproteins, liposomes, and micelles are all types of novel drug delivery system. The purpose of the present study was to formulate effective artesunate liposomal formulations. Artesunate, a lipophilic drug having short half life of 2-3hrs after oral administration which is used for the treatment of malaria, was encapsulated in micro-size liposomes. Thin film hydration method was used for the preparation of Artesunate encapsulated conventional and PEGylated liposomal suspensions. In this study, PEGylated and conventional liposomes containing Artesunate were prepared using various drug:lipid ratio and their characteristics, such as particle size, zeta potential, encapsulation efficiency, and in-vitro drug release were studied. The drug encapsulation efficiency of PEGylated liposomes was high when compared to conventional liposomes. The average particle size of both conventional and PEGylated liposomes was obtained in micrometers with PDI ranging from 0.095-0.356. Zeta potential of conventional liposomes was found to be more negative when compared to PEGylated liposomes. In-vitro drug diffusion studies was carried for period of 16 hrs where PEGylated liposomal formulation showed more sustained release compared to conventional liposomes. The conventional liposomal formulations followed zero order kinetics and PEGylated liposomal formulations followed Higuchi model.

Keywords: artesunate, thin film hydration, liposomes, conventional, PEGylated.