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生物可降解5-氟尿嘧啶载药微球的制备及性能研究
引用本文:尹静波,陈红丹,罗坤,庄秀丽,陈学思,曹田.生物可降解5-氟尿嘧啶载药微球的制备及性能研究[J].高等学校化学学报,2005,26(6):1174-1176.
作者姓名:尹静波  陈红丹  罗坤  庄秀丽  陈学思  曹田
作者单位:1. 上海大学高分子材料系, 上海201800; 2. 中国科学院长春应用化学研究所, 高分子物理与化学国家重点实验室, 长春130022
摘    要:5-氟尿嘧啶(5-Fu)为水溶性嘧啶类抗代谢药,是治疗实体肿瘤的首选药物.但5-Fu毒性很大,血浆中停留半衰期t1/2仅为10~20min.为了减少氟尿嘧啶的毒副作用并提高药物利用率,可以将其制成聚合物载药微球.聚酯类高分子是较为常用的生物降解型药物载体材料,其中聚乳酸(PLA)及其共聚物具有良好的生物相容性及生物可降解性,常被广泛应用于药物缓释材料,

关 键 词:5-氟尿嘧啶  聚乳酸(PLA)  乳酸-乙二醇(PLA-PEG)  微球  纳米二氧化硅  控制药物释放  
文章编号:0251-0790(2005)06-1174-03
收稿时间:2005-02-28

Preparation and Properties of Biodegradable Microspheres Containing 5-Fluorouracil
YIN Jing-Bo,CHEN Hong-Dan,LUO Kun,ZHUANG Xiu-li,CHEN Xue-Si,CAO Tian.Preparation and Properties of Biodegradable Microspheres Containing 5-Fluorouracil[J].Chemical Research In Chinese Universities,2005,26(6):1174-1176.
Authors:YIN Jing-Bo  CHEN Hong-Dan  LUO Kun  ZHUANG Xiu-li  CHEN Xue-Si  CAO Tian
Institution:1. Department of Polymer Materials, Shanghai University, Shanghai 201800, China; 2. State Key Laboratory of Polymer Physics and Chemistry, Changchun Institute of Applied Chemistry, Chinese Academy of Sciences, Changchun 130022, China
Abstract:Microspheres containing an antimetabolite drug 5-Fluorouracil were prepared from (poly(lactic) acide)(PLA) or poly(lactic acid)-polyethylene glycol(PLA-PEG) as the carrier by using a water-in-oil-in-water emulsion solvent evaporation technique. The conditions of the microspheres preparation such as polymer concentration in organic solvent, relative molecular weight of PLA-PEG and PLA/PEG mass ratio were discussed. The surface morphology and the size of the microspheres were observed by SEM. The drug content of microspheres was examined by TGA and the drug release in vitro was evaluated. According to the results, the drug content increased with the nano-silica used. The highest drug content in this study was 39.9%. The drug-release kinetics satisfied the requirements of controlled drug-release.
Keywords:5-Fluorouracil  Poly(lactic acide)(PLA)  Poly(lactic acid)-polyethylene glycol(PLA-PEG)  Microspheres  Nano-silica  Controlled drug-release
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