Methoxy poly(ethylene glycol) and ε-caprolactone amphiphilic block copolymeric micelle containing indomethacin.: II.: Micelle formation and drug release behaviours
Methoxy poly(ethylene glycol) and ε-caprolactone amphiphilic block copolymeric micelle containing indomethacin.: II.: Micelle formation and drug release behaviours
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DOI：
10.1016/s0168-3659(97)00124-7
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发表时间：
1998-01-23
影响因子：
10.8
通讯作者：
Sung, YK
中科院分区：
文献类型：
--
作者：
Kim, SY;Shin, ILG;Sung, YK
以甲氧基聚乙二醇（MePEG）为引发剂，通过ε-己内酯（ε-CL）的聚合反应，制备了由MePEG和ε-CL组成的两亲性嵌段共聚物。采用透析法制备了含吲哚美辛（IMC）的MePEG/ε-CL嵌段共聚物胶束，并对其作为新型药物载体的性能进行了评价。形成的胶束粒径小于200 nm，胶束粒径分布呈窄的单分散单峰型。此外，通过透析方法形成的胶束表现出球形结构。对于使用分子量为约12000且聚合物/IMC重量比为1/1的共聚物制备的那些，纳米球中的吲哚美辛含量为约42.2%。吲哚美辛从纳米球的释放速率缓慢，因此释放持续超过15天。随着共聚物分子量和包封量的增加，释放速率降低。这些结果表明，载药纳米球可以作为一种新型的药物载体，在注射给药系统的疏水性药物。(C)1998年Elsevier Science B.V.
Amphiphilic diblock copolymer composed of methoxy poly(ethylene glycol) (MePEG) and epsilon-caprolactone (epsilon-CL) was prepared by polymerization of epsilon-CL initiated with MePEG. MePEG/epsilon-CL block copolymeric micelles containing indomethacin (IMC) were prepared by a dialysis method and evaluated as a novel drug carrier. The size of micelle formed was less than 200 nm, and the size distribution of the micelle showed a narrow and monodisperse unimodal pattern. Also, the micelles formed by a dialysis method exhibited spherical structures. The indomethacin content in nanospheres was about 42.2%, for those prepared using copolymer, having molecular weight of about 12000 and polymer/IMC weight ratio of 1/1. A release rate of indomethacin from nanospheres was slow, and thus the release continued over 15 days. As the molecular weights of the copolymer and the amount of drug entrapped increased, the release rate decreased. These results indicated that the drug-loaded nanospheres could be useful as a novel drug carrier in injectable delivery systems for hydrophobic drugs. (C) 1998 Elsevier Science B.V.