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pH敏感两亲性嵌段共聚物胶束的制备及其负载紫杉醇体外药效的研究

DOI: 10.11777/j.issn1000-3304.2015.15031, PP. 1100-1106

Keywords: 两亲性嵌段共聚物,胶束,pH敏感性,紫杉醇,细胞毒性

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Abstract:

采用可逆加成-断裂链转移(RAFT)聚合法,以丙烯酸(AA)、丙烯酸异丁酯(IBA)无规共聚物与聚丙烯酸-2-羟丙酯(PHPA)反应,制备了具有pH敏感性的两亲性嵌段共聚物(P(IBA-co-AA)-b-PHPA).用红外光谱(FTIR)、核磁共振(1H-NMR)、凝胶渗透色谱(GPC)对其结构进行表征.此共聚物在水溶液中可自组装形成胶束,临界胶束浓度约为2.0mg/L.由透射电子显微镜(TEM)、动态光散射(DLS)表征可知胶束为尺寸约100nm的球形颗粒;用DLS观察到胶束粒径随pH值的升高而逐渐增大.以抗癌药物紫杉醇为模型药物,研究载药胶束在模拟人体环境中的控释行为.用CellCountingKit-8(简称CCK-8)法分别研究聚合物胶束对MCF-7人乳腺癌细胞和A549人肺癌细胞的细胞毒性,并评价载药胶束在两细胞中的抗癌效果.结果表明,P(IBA-co-AA)-b-PHPA可作为包载紫杉醇的一种新型纳米材料,载药胶束的体外释放呈明显pH依赖性,且具有较好的体外抗肿瘤活性,有望成为理想的抗肿瘤药物载体.

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