Abstract

ARTEMETHER LOADED LIPOSOMES FOR ENHANCED INTESTINAL PERMEABILITY: FORMULATION DEVELOPMENT AND EVALUATION

Rita R. Lala* and Abdul Basit Shaikh

ABSTRACT

Malaria is a life threatening disease caused by parasites which are transmitted by the bite of an infected female Anopheles mosquito. One of the drug recommended in the treatment of severe multi-drug resistant malaria is artemether. However, artemether has poor oral bioavailability and short elimination half life. The objective of this study was to formulate, optimize and evaluate, both in vitro and ex vivo, an artemether loaded nanocarrier system in the form of liposomes. A statistical factorial design was used to optimize the formulation. The amount of phospholipid and cholesterol were considered as variable factors. The selected responses included entrapment efficiency and particle size. The oral liposomal formulations of Artemether were prepared by film hydration method. The optimized batch was characterized using SEM, drug release behavior, entrapment efficiency, particle size, zeta potential and ex-vivo studies. The optimized formulation showed encapsulation efficiency 63.47%. The liposomal vesicles had homogeneous size distribution with approx size 218nm. SEM photomicrographs revealed that the drug was incorporated into the phospholipid layers. The liposomal Artemether formulation offered good in-vitro release (89.24% at the end of 24 hours). The optimized formulation exhibited permeability of 70% at the end of 6 hours with respect to artemether suspension using rat intestinal model.

Keywords: Artemether, liposomes, permeability.