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可生物降解的聚(ε-己内酯)-聚(乙二醇)嵌段共聚物:表征及其作为控释系统药物载体的应用

Biodegradable poly(epsilon-caprolactone)-poly(ethylene glycol) block copolymers: characterization and their use as drug carriers for a controlled delivery system.

作者信息

Zhou Shaobing, Deng Xianmo, Yang Hua

机构信息

Chengdu Institute of Organic Chemistry, Chinese Academy of Sciences, P.O. Box 415, Chengdu 610041, People's Republic of China.

出版信息

Biomaterials. 2003 Sep;24(20):3563-70. doi: 10.1016/s0142-9612(03)00207-2.

Abstract

Poly(epsilon-caprolactone)-poly(ethylene glycol) (PECL) copolymers were synthesized from polyethylene glycol (PEG) and epsilon-caprolactone (epsilon-CL) using stannous octoate as catalyst at 160 degrees C by bulk polymerization. The effect of the molecular weight of PEG and the copolymer ratio on the properties of the copolymers was investigated by (1)H-NMR, IR, DSC and GPC. PCL and PECL microspheres containing human serum albumin were elaborated by solvent extraction method based on the formation of double w/o/w emulsion. Microspheres were characterized in terms of morphology, size, loading efficiency, and the efficiency of microspheres formation. The results show that the microspheres prepared from PECL-10 and PECL-15 copolymers achieved the highest loading efficiency (about 50%) among all copolymers. These results indicate that the properties of copolymers could be tailored by adjusting polymer composition. It is suggested that these matrix polymers may be optimized as carriers in the protein (antigen) delivery system for different purposes.

摘要

以辛酸亚锡为催化剂,通过本体聚合法在160℃下由聚乙二醇(PEG)和ε-己内酯(ε-CL)合成了聚(ε-己内酯)-聚(乙二醇)(PECL)共聚物。通过¹H-NMR、IR、DSC和GPC研究了PEG分子量和共聚物比例对共聚物性能的影响。基于双w/o/w乳液的形成,采用溶剂萃取法制备了含人血清白蛋白的PCL和PECL微球。对微球的形态、尺寸、载药效率和微球形成效率进行了表征。结果表明,在所有共聚物中,由PECL-10和PECL-15共聚物制备的微球载药效率最高(约50%)。这些结果表明,共聚物的性能可以通过调整聚合物组成来定制。建议这些基质聚合物可针对不同目的优化作为蛋白质(抗原)递送系统中的载体。

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