Abstract
To tackle chloroquine-resistant Plasmodium parasites, the characteristics of conventional medicines should be improved. Halofantrine (HF) is one such successful drug that is used to treat malaria. However, it is poorly soluble, with non-dose-proportional bioavailability, and causes cardiac side effects. In this study, HF was formulated with five different nanoformulations: nanoprecipitation suspension with two different preparation protocols (NPSI and NPSII), emulsification/solvent evaporation by high shear homogenization (ESEhsh), emulsification/solvent evaporation by tip sonication (ESEts), and nanoliposomes (NLS). ESEts nanoparticles showed a size of 100 +/- 26 nm with fair homogeneity (polydispersity index - 0.3 +/- 0.04), reasonable encapsulation efficiency (26 +/- 0.9%), high anionic charge (zeta potential = -76 +/- 3 mV), and slow-release (62 +/- 7%) within 72 h. Therefore, ESEts is a promising candidate for HF-based antimalarial drug formulations for in vivo models.