Abstract

PREPARATION AND CHARACTERIZATION OF LUMEFANTRINPEG 4000 SOLID DISPERSIONS

*Mumuni A. Momoh, Gwarzo S. Mahmud, Musiliu O. Adedokun, Mba C. Chukwuemeka and A R. Oyi

Abstract

The objective of the present investigation was to explore the potential of solid dispersions (SDs) for the oral delivery of lumefantrin, a poorly water-soluble antimalarial agent. The SDs containing LMFT were formulated by employing melt fusion technique. Five different ratios of PEG-4000 and LMFT (1:1, 1:3, 3:1, 0:1 and 1:0) were prepared. The SDs was evaluated for particle size, encapsulation efficiency, in vitro drug release. The antimalarial activity of SDs formulated was evaluated in Plasmodium berghei infected mice. Thermograms of the SDs showed modifications in the peaks. Particle sizes of SDs were depend on the ratio of the PEG and drug. The SDs had high drug content and showed sustained release capability as compared to marketed sample. In vivo pharmacodynamic studies showed that LMFT-SDs exhibited significantly higher antimalarial activity (P < 0.05) as compared to the marketed formulation. LMFT-SDs is comparatively better with respect to antimalarial effect, sustained release and survival rate of the animal than marketed sample.

Keywords: lumefantrin, solid dispersion, anti-malaria.