Studies on the Preparation and Evaluation of Antimalarial activity of Arteether and Complexed Arteether with β-CD Loaded Chitosan/Lecithin Nanoparticles

Sushma      Gupta; Renu      Chadha

Abstract

The present work explores the preparation and characterization of chitosan/lecithin nanoparticles loaded with arteether (ART) and arteether entrapped in cyclodextrins (ART-β CD) to boost its anti-malarial activity. Arteether, an antimalarial drug was chosen by the Steering Committee of the Scientific Working Group on Malaria Chemotherapy of the WHO (CHEMAL) for treatment of cerebral malaria. Unfortunately, ART is water-insoluble drug (17µg/ml at room temp.) and its therapeutic efficacy is greatly hampered due to poor bioavailability (~40%, degradation in stomach acids). Moreover, Arteether have short plasma half-life which requires frequent administration. Formation of nanoparticles of ART can be a suitable solution to improve their Biopharmaceutical properties. The nanoparticles prepared using modified solvent evaporation method depicted a particle size in the range of 299-354 nm for arteether and 157-212 nm for ART-β CD loaded nanoparticles. 100mg loaded ART and ART-β CD formulations showed maximum drug entrapment efficiency. Prepared nanoparticles reflected spherical shape inTEM images. Disappearance of decomposition endotherm in DSC scans of nanoparticles revealed the increased physical stability. FT-IR spectra showed small changes in major peaks of drug negating any chemical change in the drug when entrapped in the nanoparticle formulation. In vitro drug release studies suggested the controlled release as well as improved pattern. Enhanced antimalarial activity was observed in ART and ART-β CD containing nanoparticles.

Keywords: Arteether, β-cyclodextrin, entrapment efficiency, in vivo anti-malarial activity, nanoparticles.

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