Kim S Y, Shin I G, Lee Y M, Cho C S, Sung Y K
Department of Industrial Chemistry, College of Engineering, Hanyang University, Seoul, Korea.
J Control Release. 1998 Jan 23;51(1):13-22. doi: 10.1016/s0168-3659(97)00124-7.
Amphiphilic diblock copolymer composed of methoxy poly(ethylene glycol) 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 12,000 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.
以甲氧基聚（乙二醇）（MePEG）引发ε-己内酯（ε-CL）聚合制备了由甲氧基聚（乙二醇）和ε-己内酯（ε-CL）组成的两亲性二嵌段共聚物。通过透析法制备了载有吲哚美辛（IMC）的MePEG/ε-CL嵌段共聚物胶束，并将其作为一种新型药物载体进行了评价。形成的胶束尺寸小于200nm，胶束的尺寸分布呈现出窄且单分散的单峰模式。此外，通过透析法形成的胶束呈现出球形结构。对于使用分子量约为12000且聚合物/IMC重量比为1/1的共聚物制备的纳米球，吲哚美辛含量约为42.2%。吲哚美辛从纳米球中的释放速率较慢，因此释放持续超过15天。随着共聚物分子量和包封药物量的增加，释放速率降低。这些结果表明，载药纳米球可作为疏水性药物注射给药系统中的新型药物载体。
