Brush-like amphiphilic copolymers based on polylactide and poly(ethylene glycol): Synthesis, self-assembly and evaluation as drug carrier

Brush-like amphiphilic copolymers based on polylactide and poly(ethylene glycol): Synthesis, self-assembly and evaluation as drug carrier
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DOI:
10.1016/j.polymer.2013.01.042
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发表时间:
2013-03
期刊:
影响因子:
4.6
通讯作者:
Youssef Bakkour;V. Darcos;Fanny Coumes;Suming Li;J. Coudane
Youssef Bakkour;V. Darcos;Fanny Coumes;Suming Li;J. Coudane
中科院分区:
化学2区
文献类型:
--
作者:
Youssef Bakkour;V. Darcos;Fanny Coumes;Suming Li;J. Coudane

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采用开环聚合(ROP)和原子转移自由基聚合(ATRP)相结合的方法合成了一系列新型两亲性聚(聚乙二醇甲基丙烯酸酯)-嵌段-聚(L-丙交酯)-嵌段-聚(聚乙二醇甲基丙烯酸酯)(P(PEGMA)-b-PLLA-b-P(PEGMA))共聚物。首先,通过使用双官能引发剂的l-丙交酯的ROP,以及随后的羟基端基与2-溴异丁酰溴的反应,分两步制备两种α,ω-遥爪PLLA ATRP大分子引发剂。然后,使用PLLA大分子引发剂进行聚(乙二醇)甲基丙烯酸酯的ATRP。用1H NMR、体积排阻色谱和DOSY NMR对产物进行了表征。用荧光光谱、动态光散射和透射电镜研究了共聚物在水溶液中的聚集行为。临界聚集浓度在0.08-0.12 g L-1的范围内。通过DLS测定的纳米颗粒(NP)的直径约为100 nm。TEM图像显示,这些纳米尺寸的物体是球形的。对疏水模型药物氯法齐明的初步研究表明,这种纳米粒可能成为潜在的药物传递载体。
A series of novel amphiphilic poly(poly(ethylene glycol) methacrylate)-block-poly(l-lactide)-block-poly(poly(ethylene glycol) methacrylate) (P(PEGMA)-b-PLLA-b-P(PEGMA)) copolymers were synthesized by combination of ring-opening polymerization (ROP) and atom transfer radical polymerization (ATRP). First, two α,ω-telechelic PLLA ATRP macroinitiators were prepared in two steps via ROP of l-lactide using a difunctional initiator, and subsequent reaction of the hydroxyl end groups with 2-bromoisobutyryl bromide. Then, the ATRP of poly(ethylene glycol) methacrylate was carried out using PLLA macroinitiators. The resulting brush-like triblock copolymers were characterized by1H NMR, size exclusion chromatography and DOSY NMR. The aggregation behavior of the copolymers in aqueous medium was investigated by fluorescence spectroscopy, dynamic light scattering (DLS), and transmission electron microscopy (TEM). The critical aggregation concentration was in the range of 0.08–0.12 g L−1. The diameter of the nanoparticles (NPs), determined by DLS, was around 100 nm. TEM images showed that these nano-sized objects were spherical in shape. Preliminary studies with a hydrophobic model drug, namely clofazimine, exhibited that such NPs could be potential candidates for drug delivery carrier.