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首页> 外文期刊>Journal of Applied Polymer Science >Self-assembled micelles prepared from poly(epsilon-caprolactone)-poly(ethylene glycol) and poly(epsilon-caprolactone/glycolide)-poly(ethylene glycol) block copolymers for sustained drug delivery
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Self-assembled micelles prepared from poly(epsilon-caprolactone)-poly(ethylene glycol) and poly(epsilon-caprolactone/glycolide)-poly(ethylene glycol) block copolymers for sustained drug delivery

机译：由聚（ε-己内酯） - 聚（乙二醇）和聚（ε-己内酯/乙酰胺） - 聚（乙二醇）嵌段共聚物来制备自组装胶束 - 用于持续的药物递送

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A series of poly(epsilon-caprolactone)-poly(ethylene glycol) (PCL-PEG) and poly(epsilon-caprolactone/glycolide)-poly(ethylene glycol) [P(CL/GA)-PEG] diblock copolymers were prepared by ring-opening polymerization of E-caprolactone or a mixture of E-caprolactone and glycolide using monomethoxy PEG (mPEG) as macroinitiator and Sn(Oct)(2) as catalyst. The resulting copolymers were characterized using 1 H-NMR, gel permeation chromatography, differential scanning calorimetry, and wide-angle X-ray diffraction. Copolymer micelles were prepared using the nanoprecipitation method. The morphology of the micelles was spherical or wormlike as revealed by transmission electron microscopy, depending on the copolymer composition and the length of the hydrophobic block. Introduction of the glycolide component, even in small amounts (CL/GA=10), disrupted the chain structure and led to the formation of spherical micelles. Interestingly, the micelle size decreased with the encapsulation of paclitaxel. Micelles prepared from mPEG5000-derived copolymers exhibited better drug loading properties and slower drug release than those from mPEG2000-derived copolymers. Drug release was faster for copolymers with shorter PCL blocks than for those with longer PCL chains. The introduction of glycolide moieties enhanced drug release, but the overall release rate did not exceed 10% in 30 days. In contrast, drug release was enhanced in acidic media. Therefore, these bioresorbable micelles and especially P(CL/GA)-PEG micelles with excellent stability, high drug loading content, and prolonged drug release could be promising for applications as drug carriers. (C) 2017 Wiley Periodicals, Inc.
机译：一系列聚（ε-己内酯） - 聚（乙二醇）（PCL-PEG）和聚（ε-己内酯/乙酰基） - 聚（乙二醇）[P（Cl / Ga）-PEG]二嵌段共聚物制备二嵌段共聚物E-己内酯的开环聚合或E-己内酯和乙酰胺的混合物，使用单甲氧基PEG（MPEG）作为大型灭菌剂和Sn（OCT）（2）作为催化剂。使用1 H-NMR，凝胶渗透色谱，差示扫描量热法和广角X射线衍射来表征所得共聚物。使用纳米沉淀方法制备共聚物胶束。通过透射电子显微镜透露，胶束的形态是球形或蠕虫，取决于共聚物组合物和疏水性嵌段的长度。乙酰胺组分的引入，即使少量（Cl / Ga = 10），破坏链结构并导致球形胶束。有趣的是，胶束尺寸随着紫杉醇的封装而降低。由MPEG5000衍生的共聚物制备的胶束表现出比来自MPEG2000衍生的共聚物的药物释放更好的药物负载性能和较慢的药物释放。对于具有较长的PCL链块的共聚物，药物释放比对于具有较长的PCL链条的共聚物更快。乙醇胺部分引入增强药物释放，但总释放速率在30天内不超过10％。相比之下，在酸性介质中提高了药物释放。因此，这些可生物可吸收的胶束和尤其是具有优异稳定性，高药物负载含量和延长药物释放的PEG（CL / GA）-PEG胶束可以对药物载体的应用可能是有望的。 （c）2017 Wiley期刊，Inc。

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