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伯氨喹基于红细胞的递送系统:体外特性研究

Erythrocyte based delivery system of primaquine: in vitro characterization.

作者信息

Talwar N, Jain N K

机构信息

Department of Pharmaceutical Sciences, Sagar, India.

出版信息

J Microencapsul. 1992 Jul-Sep;9(3):357-64. doi: 10.3109/02652049209021250.

Abstract

Primaquine phosphate, an antimalarial drug, was loaded in erythrocytes by the process of endocytosis. The encapsulation of 0.1-0.15 mg of drug ml-1 of packed erythrocytes was achieved. The loaded cells attained spherical shape and exhibited higher osmotic fragility and lower resistance to turbulence shock as compared with normal cells. Glutaraldehyde treatment stabilized the cells which were noted to be resistant to the osmotic and turbulence shocks. In vitro release of drug and haemoglobin was also retarded upon treatment of loaded erythrocytes with glutaraldehyde. The studies suggest the potentiality of primaquine-loaded, glutaraldehyde-treated erythrocytes as an intravenous drug delivery system for casual prophylaxis and radical cure of malaria.

摘要

磷酸伯氨喹是一种抗疟药物,通过内吞作用被载入红细胞。实现了每毫升压积红细胞载入0.1 - 0.15毫克药物。载入药物的细胞呈球形,与正常细胞相比,表现出更高的渗透脆性和更低的抗湍流冲击能力。戊二醛处理使细胞稳定,这些细胞被观察到对渗透和湍流冲击具有抗性。用戊二醛处理载入药物的红细胞后,药物和血红蛋白的体外释放也受到抑制。这些研究表明,载入伯氨喹并经戊二醛处理的红细胞作为一种静脉给药系统用于疟疾的临时预防和根治具有潜力。

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