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

被引:7
|
作者
Chinaeke, Eric E. [1 ]
Chime, Salome A. [2 ]
Ogbonna, John D. N. [1 ]
Attama, Anthony A. [1 ]
Mueller-Goymann, C. C. [3 ]
Okore, Vincent C. [1 ]
机构
[1] Univ Nigeria, Dept Pharmaceut, Nsukka 410001, Nigeria
[2] Univ Nigeria, Dept Pharmaceut Technol & Ind Pharm, Nsukka 410001, Nigeria
[3] Tech Univ Carolo Wilhelmina Braunschweig, Inst Pharmazeut Technol, D-38106 Braunschweig, Germany
关键词
IV-IVC; artesunate; dika wax; lipospheres; soybean oil; structured lipid matrices; DRUG-DELIVERY SYSTEMS; PLASMODIUM-FALCIPARUM; LIPID MATRICES; THEOBROMA OIL; CAPRA-HIRCUS; RELEASE; LONG; BIOAVAILABILITY; ARTEMISININ; MALARIA;
D O I
10.3109/02652048.2014.940008
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
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.
引用
收藏
页码:796 / 804
页数:9
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