Chinaeke E.E., Chime S.A., Ogbonna J.D.N., Attama A.A., Müller-Goymann C.C., Okore V.C.
Department of Pharmaceutics, University of Nigeria, Nsukka, Nigeria; Department of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria, Nsukka, Nigeria; Institut für Pharmazeutische Technologie, Technische Universität Carolo-Wilhelmin
Chinaeke, E.E., Department of Pharmaceutics, University of Nigeria, Nsukka, Nigeria; Chime, S.A., Department of Pharmaceutical Technology and Industrial Pharmacy, University of Nigeria, Nsukka, Nigeria; Ogbonna, J.D.N., Department of Pharmaceutics, University of Nigeria, Nsukka, Nigeria; Attama, A.A., Department of Pharmaceutics, University of Nigeria, Nsukka, Nigeria; Müller-Goymann, C.C., Institut für Pharmazeutische Technologie, Technische Universität Carolo-Wilhelmina zu Braunschweig, Braunschweig, Germany; Okore, V.C., Department of Pharmaceutics, University of Nigeria, Nsukka, Nigeria
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 A˚ while, wide angle X-ray diffraction (WAXD) showed prominent reflection at 2θ = 20.83°, d = 0.42 A˚. 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. © 2014 Informa UK Ltd.
artesunate; dika wax; lipid; liposphere; phospholipid; soybean oil; unclassified drug; wax; antimalarial agent; artemisinin derivative; artesunate; dika fat; liposome; soybean oil; vegetable oil; animal experiment; area under the curve; Article; controlled study; correlational study; drug absorption; drug bioavailability; drug delivery system; drug formulation; drug solubility; drug stability; encapsulation; in vitro study; in vivo study; nonhuman; particle size; rat; small angle X ray diffraction; sustained drug release; tablet; wide angle X ray diffraction; X ray diffraction; animal; chemistry; evaluation study; female; malaria; male; oral drug administration; pH; Wistar rat; Administration, Oral; Animals; Antimalarials; Artemisinins; Female; Hydrogen-Ion Concentration; Liposomes; Malaria; Male; Plant Oils; Rats; Rats, Wistar; Soybean Oil
