Bio-inspired artemether-loaded human serum albumin nanoparticles for effective control of malaria-infected erythrocytes

Nanomedicine (Lond). 2016 Nov;11(21):2809-2828. doi: 10.2217/nnm-2016-0235. Epub 2016 Oct 19.

Abstract

Aim: The intra-erythrocytic development of the malarial parasite is dependent on active uptake of nutrients, including human serum albumin (HSA), into parasitized red blood cells (pRBCs). We have designed HSA-based nanoparticles as a potential drug-delivery option for antimalarials.

Methods: Artemether-loaded nanoparticles (AANs) were designed and antimalarial activity evaluated in vitro/in vivo using Plasmodium falciparum/Plasmodium berghei species, respectively.

Results: Selective internalization of AAN into Plasmodium-infected RBCs in preference to healthy erythrocytes was observed using confocal imaging. In vitro studies showed 50% dose reduction for AAN as compared with drug-only controls to achieve IC50 levels of inhibition. The nanoparticles exhibited twofold higher peak drug concentrations in RBCs with antimalarial activity at 50% of therapeutic doses in P. bergei infected mice.

Conclusion: Novel HSA-based nanoparticles offer safe and effective approach for selective targeting of antimalarial drugs.

Keywords: artemether; human serum albumin nanoparticles; malaria; parasitized RBCs.