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 2 theta = 2.49 degrees, d = 3.55 angstrom while, wide angle X-ray diffraction (WAXD) showed prominent reflection at 2 theta = 20.83 degrees, d = 0.42 angstrom. 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.