短嵌段长度甲氧基聚（乙二醇）-嵌段-聚（己内酯）二嵌段共聚物的合成与胶束表征

Synthesis and micellar characterization of short block length methoxy poly(ethylene glycol)-block-poly(caprolactone) diblock copolymers.

作者信息

Letchford Kevin, Zastre Jason, Liggins Richard, Burt Helen

机构信息

Faculty of Pharmaceutical Sciences, University of British Columbia, 2146 East Mall, Vancouver, B.C., Canada V6T 1Z3.

出版信息

Colloids Surf B Biointerfaces. 2004 May 15;35(2):81-91. doi: 10.1016/j.colsurfb.2004.02.012.

DOI:10.1016/j.colsurfb.2004.02.012

PMID:15261040

Abstract

A series of short block length methoxy poly(ethylene glycol)-block-poly(caprolactone) diblock copolymers was synthesized and characterized in order to assess the potential of these copolymers as a micellar drug-delivery system. Varying the caprolactone:MePEG weight ratio in the reaction mixture allowed the synthesis of diblock copolymers with a MePEG molecular weight of 750 g/mol and PCL block lengths of 2, 5 or 10 repeat units. Phase diagrams of aqueous solutions of the copolymers were constructed which displayed characteristic cloud points and Krafft points. As the degree of polymerization of PCL increased, critical micelle concentration (CMC) values decreased from 6.97 x 10(-1) to 3.38 x 10(-3) g/l, partition equilibrium coefficients (Kv) increased from 1.09 x 10(4) to 22.2 x 10(4),and hydrodynamic diameters increased from 12.2 to 19.5 nm. The micelle morphology was determined to be spherical by transmission electron microscopy.

摘要

合成并表征了一系列短嵌段长度的甲氧基聚（乙二醇）-嵌段-聚（己内酯）二嵌段共聚物，以评估这些共聚物作为胶束药物递送系统的潜力。通过改变反应混合物中己内酯与甲氧基聚乙二醇（MePEG）的重量比，可以合成MePEG分子量为750 g/mol且聚己内酯（PCL）嵌段长度为2、5或10个重复单元的二嵌段共聚物。构建了共聚物水溶液的相图，这些相图显示出特征性的浊点和克拉夫特点。随着PCL聚合度的增加，临界胶束浓度（CMC）值从6.97×10⁻¹降至3.38×10⁻³ g/l，分配平衡系数（Kv）从1.09×10⁴增至22.2×10⁴，流体力学直径从12.2增至19.5 nm。通过透射电子显微镜确定胶束形态为球形。