Evaluation of dika wax-soybean oil-based artesunate-loaded lipospheres: in vitro–in vivo correlation studies

Abstract

Objectives: To formulate and evaluate artesunate-loaded lipospheres and study the in vitro–in vivo correlations (IV-IVC). Materials and methods: Lipospheres were formulated by melt homogenisation using structured lipid matrices consisting of (1:3 and 1:6) soybean oil and dika wax and were characterised in vitro and in vivo. Results: The small angle X-ray diffraction (SAXD) results of the lipid matrices showed prominent reflection at 2θ = 2.49°, d = 3.55 Å while, wide angle X-ray diffraction (WAXD) showed prominent reflection at 2θ = 20.83°, d = 0.42 Å. Lipospheres had maximum encapsulation efficiency of 80%, showed no significant decrease in pH with time (p < 0.05), and had sustained release properties. The ratio of the area under the curve (AUC) of the lipospheres and the tablets gave bioavailability enhancement factor of 2.108. Conclusion: Artesunate-loaded lipospheres could be used orally or parenterally once daily, for the treatment of malaria.

• IV-IVC
• artesunate
• dika wax
• lipospheres
• soybean oil
• structured lipid matrices

Acknowledgements

The authors wish to thank Ursula Jahn of Technical University of Braunschweig, for X-ray analysis and Emzor Pharmaceutical Limited, Lagos, Nigeria for providing samples of artesunate used for this study. We also wish to thank Alexander von Humboldt Foundation, Bonn-Bad Godesberg Germany, for donating some of the equipment used in this work.