Preparation and characterization of polymer micelles from poly(ethylene glycol)-poly(D,L-lactide) block copolymers as potential drug carrier
Preparation and characterization of polymer micelles from poly(ethylene glycol)-poly(D,L-lactide) block copolymers as potential drug carrier
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DOI：
10.1016/s0168-3659(99)00028-0
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发表时间：
1999-11-01
影响因子：
10.8
通讯作者：
Kataoka, K
中科院分区：
文献类型：
--
作者：
Yasugi, K;Nagasaki, Y;Kataoka, K
以环氧乙烷和D，L-丙交酯为原料，采用阴离子引发剂连续开环聚合，制备了不同组成的聚乙二醇聚(D，L-丙交酯)嵌段共聚物，并从疏水药物载体设计的角度详细考察了它们在水溶液中的多分子胶束性质。研究发现，聚乙二醇聚乳酸的非均质性对胶束的大小和分布有重要影响，只有聚乙二醇聚乳酸的相对分子质量分布较窄，聚乙二醇聚乳酸的链段长度与聚乙二醇聚乳酸链段的长度比达到适当的平衡，才能形成直径接近30 nm的窄分布胶束，这表明为嵌段共聚物建立一条可靠的合成路线是非常重要的。聚乙二醇聚乳酸胶束具有相当低的临界结合浓度(接近1 mg/L)，这显然是在极度稀释的条件下利用这些胶束作为药物载体的优势。(C)1999 Elsevier Science B.V.保留所有权利。
Poly(ethylene glycol)-poly(D,L-lactide) block copolymers (PEG-PLA) with varying composition were prepared through successive ring-opening polymerization of ethylene oxide and D,L-lactide using an anionic initiator, and their property of multimolecular micellization in aqueous milieu was examined in detail from the standpoint of designing carriers for hydrophobic drugs. The heterogeneity of PEG-PLA was found to crucially affect the size and distribution of micelles, and narrowly-distributed micelles with sizes of similar to 30 nm in diameter were formed only from PEG-PLA with a substantially narrow molecular weight distribution and an appropriate balance in the length ratio of the PEG and PLA segments in PEG-PLA, indicating the importance of establishing a reliable synthetic route for the block copolymers. PEG-PLA micelles have a considerably low critical association concentration (similar to 1.0 mg/l) which is apparently an advantage in utilizing these micelles as drug carriers in an extremely diluted condition. (C) 1999 Elsevier Science B.V. All rights reserved.