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    聚乳酸-聚乙二醇嵌段共聚物胶束的制备及性能研究

    Preparation and Properties of Polylactide-Poly(ethylene glycol) Block Copolymer Micelles

    • 摘要: 分别以聚乙二醇(PEG)及聚乙二醇单甲醚(mPEG)引发L-丙交酯开环聚合得到PLLA(聚乳酸)-PEG-PLLA三嵌段与PLLA-mPEG两嵌段共聚物,通过1H-NMR分析确定共聚物的结构及分子量。采用直接溶解法和有机溶剂挥发法制备PLLA-PEG-PLLA及PLLA-mPEG胶束,并用TEM对其形态进行表征。利用激光粒度分析和染料探针的方法证实了共聚物自组装形成了胶束,且具有较小的临界胶束浓度(CMC),粒径约为100 nm。三嵌段PLLA-PEG-PLLA胶束的粒径小于两嵌段PLLA-mPEG胶束的粒径;有机溶剂挥发法制备的胶束粒径小于直接溶解法制备的胶束粒径。盐酸乌拉地尔胶束的体外释放结果表明,共聚物组成以及载药方式等对胶束载药、释药行为有一定影响,胶束对所包载的盐酸乌拉地尔具有明显的缓释作用。

       

      Abstract: PLLA-PEG-PLLA and PLLA-mPEG copolymers were synthesized via ring-opening polymerization of L-lactide using polyethylene glycol and methoxypolyethylene glycols as initiators, respectively. Their structures and molecular weights were characterized by 1H-NMR. Micelles were prepared by direct dissolution or organic solvent evaporation, and the morphology and properties of the micelles were determined by TEM, DLS and dye probe techniques. The micelles formed have low CMC and are spherical in shape with sizes around 100 nm. The micellar diameter strongly depends on copolymer composition. The diameter of PLLA-PEG-PLLA micelles is smaller than that of PLLA-mPEG micelles, and solvent evaporation can result in smaller micelle size than direct dissolution. The in vitro study of Urapidil hydrochloride release indicates that drug loading efficiency and drug releasing rate are related to copolymer composition and preparation methods. The micelles show excellent sustained-release capability for Urapidil hydrochloride.

       

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