Enhanced antimalarial activity of lumefantrine nanopowder prepared by wet-milling DYNO MILL technique

Abstract

Lumefantrine (LMF) is an antimalarial drug that exhibits poor oral bioavailability, owing to its poor aqueous solubility. To improve its antimalarial activity, nanopowder formulation using DYNO MILL was prepared. Combination of HPMC E3 (4%, w/v) and Tween 80 (2.5%, w/v) as dispersing agents, favored the production of smaller LMF particles with mean size of 0.251μm. LMF nanopowder showed enhanced dissolution rate attributed to nanonization of LMF. The IC 50 value of nano-sized LMF was found to be 0.1ng/mL, which was 175-times lower than the IC 50 value of unmilled LMF powder (17.5ng/mL) and 42-times lower than the IC 50 value of chloroquine (4.2ng/mL). The in vivo antimalarial activity demonstrated an enhanced antimalarial potential of LMF nanopowder against P. Yoelii nigeriensis compared to unmilled drug. Wet-milling using DYNO MILL offers a highly effective approach to produce stable drug nanopowders. Furthermore, LMF nanopowder makes the Coartem ® therapy more effective. © 2012 Elsevier B.V..