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以异辛酸亚锡为催化剂,通过四臂聚乙二醇(4-armed PEG)引发右旋丙交酯(DLA)或左旋丙交酯(LLA)开环聚合合成四臂PEG-PLA对映体共聚物.通过纳米沉淀的方法制备了四臂PEG-b-PDLA胶束(PDM)、四臂PEG-b-PLLA胶束(PLM)和四臂PEG-b-PDLA/四臂PEG-b-PLLA立体复合胶束(SCM),并对其形貌、粒径、稳定性和立体复合机理等进行系统表征.以阿霉素(DOX)为模型抗肿瘤药物载入胶束中,与PDM和PLM相比,SCM具有更优异的药物负载能力.与DOX相比,载药四臂PEG-PLA胶束,尤其是负载DOX的SCM,表现出更优异的肿瘤细胞增殖抑制效果,作用更持久,并且对正常细胞的毒性较小,从而揭示了其作为潜在抗肿瘤药物载体的良好前景.
Four-arm PEG-PLA enantiomer was synthesized by four-arm PEG-initiated dextran (DLA) or L-lactide (LLA) ring opening polymerization using stannous octoate as a catalyst Copolymers were prepared by four-arm PEG-b-PDLA micelles (PDM), four-arm PEG-b-PLLA micelles (PLM) and four arm PEG-b-PDLA / PLLA stereocomplex micelles (SCMs) were synthesized and characterized by morphology, particle size, stability and stereocomplex mechanism.Doxorubicin (DOX) was used as a model to load the antitumor drug into the micelles, PLM.Compared with DOX, drug-loaded four-arm PEG-PLA micelles, especially DOX-loaded SCM, showed more excellent tumor cell proliferation inhibitory effect, longer lasting effect, And less toxic to normal cells, revealing a promising future as a potential antitumor drug carrier.