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J Microencapsul ; 31(8): 796-804, 2014.
Article in English | MEDLINE | ID: mdl-25090593

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.


Subject(s)
Antimalarials , Artemisinins , Malaria/drug therapy , Plant Oils , Soybean Oil , Administration, Oral , Animals , Antimalarials/chemistry , Antimalarials/pharmacology , Artemisinins/chemistry , Artemisinins/pharmacology , Artesunate , Female , Hydrogen-Ion Concentration , Liposomes , Male , Plant Oils/chemistry , Plant Oils/pharmacology , Rats , Rats, Wistar , Soybean Oil/chemistry , Soybean Oil/pharmacology
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