Preparation, characterisation and in vitro/in vivo anticancer activity of lyophilised artesunate-loaded nanoparticles

An antimalarial drug, artesunate (ART), has been recently investigated as a potential anticancer agent. The aim of the present study was to develop novel surface-engineered ART-loaded nanoparticles (NPs) (a lyophilised powder for parenteral injection) possessing an enhanced stability and biological activity. The NPs were com-posed of poly(lactic-co-glycolic) acid (PLGA) as a carrier polymer and PLGA-polyethylene glycol (PEG) as a surface-engineering (PEGylation) co-polymer. The lyophilised nanosuspension of the ART-loaded NPs showed spherical spongy-cake like appearance, and the ART-loaded NPs presented a smooth surface and a particle size of about 200 nm. ART in the lyophilised NPs was in an amorphous state showing a biphasic drug release profile in vitro. The ART-loaded PEGylated NPs were shown to be physically stable for at least 12 months at 5 +/- 3 degrees C. The ART-loaded NPs exhibited an enhanced inhibitory effect (over a free drug, p < 0.05) on Lewis lung carcinoma (LLC) cells and in tumour bearing mice at a dose of 60 mg/kg/day (i.v.) within a 14-day study period. In conclusion, the present PEGylated and PLGA-based ART-loaded NPs could be applicable as a potential drug delivery system for anticancer drug treatment purposes.