Department of Chemistry and Bioengineering, Faculty of Engineering, Iwate University, 4-3-5 Ueda, Morioka, Iwate 020-8551, Japan.
Biomacromolecules. 2013 Jul 8;14(7):2171-8. doi: 10.1021/bm400275w. Epub 2013 Jun 6.
This paper describes the one-pot synthesis of a polyglycidol (PG)-based polymer, poly(ethoxyethyl glycidyl ether) (PEEGE)-b-[hyperbranched polyglycerol (hbPG)-co-PEEGE]x/y, its micelle formulation, and the ability to encapsulate a model therapeutic molecule. Amphiphilic block copolymers were prepared by the sequential addition of ethoxyethyl glycidyl ether (EEGE) to glycidol. The composition of the block copolymers varied from 62:38 to 92:8. Block copolymers with composition x:y≥66:34 were soluble only in organic solvents. Micelles were formulated by injection of deionized water into a tetrahydrofuran block copolymer solution with or without pyrene as a model hydrophobic molecule. The critical micelle concentration was 18.2-30.9 mg/L, and the micelle size was 100-250 nm. The pyrene-containing micelle rapidly collapsed on acidic exposure, allowing conversion of hydrophobic PEEGE to hydrophilic PG, thus, facilitating the release of the encapsulated pyrene. Cytotoxicity data showed high biocompatibility of PG-based block copolymers, suggesting their potential as a drug delivery carrier.
本文描述了一种聚环氧乙烷（PG）基聚合物，聚（乙氧基乙基环氧乙烷）（PEEGE）-b-[超支化聚甘油（hbPG）-co-PEEGE]x/y 的一锅法合成、胶束制剂及其封装模型治疗分子的能力。两亲性嵌段共聚物通过乙氧基乙基缩水甘油醚（EEGE）顺序添加到环氧乙烷中制备。嵌段共聚物的组成从 62:38 变化到 92:8。组成 x:y≥66:34 的嵌段共聚物仅可溶于有机溶剂。通过将去离子水注入四氢呋喃嵌段共聚物溶液中，形成或不形成芘作为模型疏水分子来制备胶束。临界胶束浓度为 18.2-30.9 mg/L，胶束尺寸为 100-250nm。含芘的胶束在酸性暴露下迅速崩溃，使疏水性 PEEGE 转化为亲水性 PG，从而有利于封装的芘的释放。细胞毒性数据表明 PG 基嵌段共聚物具有高生物相容性，表明其作为药物输送载体的潜力。
