顺铂温敏载药粒子的制备表征
Preparation and Characterization of Cisplatin-loaded Thermosensitive Micelle
作者单位
杨觅 南京大学医学院附属鼓楼医院肿瘤中心南京 210008 
丁义涛 南京大学医学院附属鼓楼医院肿瘤中心南京 210008 
黄兆琦 南京大学生命科学院南京 210093 
钱晓萍 南京大学医学院附属鼓楼医院肿瘤中心南京 210008 
禹立霞 南京大学医学院附属鼓楼医院肿瘤中心南京 210008 
刘宝瑞 南京大学医学院附属鼓楼医院肿瘤中心南京 210008 
摘要: 制备了顺铂温敏载药纳米粒子,表征其相关性质并考察不同温度下对体外肿瘤细胞的生长抑制作用。制备的两亲嵌段聚合物在水溶液中自发形成胶束结构并包裹顺铂,测定顺铂载药粒子的结构、形态、粒径及包封率、载药量、晶体状态等特性,并对顺铂的体外释放以及不同细胞系体外毒性也做了研究。载药粒子粒径为83.3 ± 4.3 nm,载药量为37.8%,包封率为77.8%。血清中相变温度39.3 ℃。载药颗粒在单纯化疗时细胞抑制率较小,加热后抑制作用明显增加(P<0.01),与游离药物相近(P>0.5)。顺铂载药纳米粒子具有较好的温控特性,为顺铂在肿瘤热靶向治疗中的应用提供了一条新的途径。
关键词: 温敏  顺铂  靶向治疗
基金项目: 
Abstract: Cisplatin-loaded thermosensitive micelle was prepared and its characters and cytotoxicity were evaluated at different temperature in vitro. The thermally sensitive block copolymer, poly(N-isopropylacrylamide-co-acrylamide)-b-poly(D,L-lactide), was synthesized by free radical polymerization and ring-opening polymerization. Cisplatin-loaded micelle was made of such thermosensitive polymer. The drug loading content was 37.8% and the entrapment efficiency was 77.8%. The LCST in serum was 39.3 ℃. The physical properties, such as structure, size distribution, crystallization and morphology of the cisplatin-loaded micelles were characterized by NMR, XRD, DLS and AFM. The efficacy of this drug delivery system was also evaluated by examining the proliferation inhibiting activity against different cell lines in vitro. The results demonstrate that this copolymer could be an ideal candidate for thermal targeted antitumor drug delivery.
Keywords: thermosensitive  cisplatin  target therapy
 
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杨觅,丁义涛,黄兆琦,钱晓萍,禹立霞,刘宝瑞.顺铂温敏载药粒子的制备表征[J].无机化学学报,2007,23(2):205-210.
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