Assessment of formulated amodiaquine microparticles in Leishmania donovani infected rats

Abstract

The aim of this study was to formulate, characterise and evaluate the activity of amodiaquine microparticles against Leishmania donovani. Microparticles were formulated by encapsulating the drug in bovine serum albumin using the spray-dryer method. The microparticles were evaluated for size, zeta potential, drug content, encapsulation efficiency and in vitro release profile. The size range of the microparticles formulated was between 1.9 and 10 μm with an average zeta potential of −25.5 mV. Of the expected 20% drug loading, an average of 18.27% was obtained giving an encapsulation efficiency of 91.35%. Pharmacokinetic profile of amodiaquine improved with microencapsulation of the drug with C_max, AUC_0→48 and t_1//2 all significantly higher than amodiaquine solution. Amodiaquine microparticles showed an overall higher bioavailability and hence were more effective in eliminating intra-tissue parasites than the drug solution. It would therefore be expected that the formulated microparticles will be more effective in treating visceral leishmaniasis.

Keywords:

• Amodiaquine; Leishmania donovani
• albumin
• microparticles
• pharmacokinetics

Acknowledgements

The entire research was funded by the Office of Research, Innovation and Development (ORID) of the University of Ghana.

Disclosure statement

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this article.

Additional information

Funding

The entire research was funded by the Office of Research, Innovation and Development (ORID) of the University of Ghana [ORID Ref#: URF/6/LMG-001/2012-2013].