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聚乙二醇支载紫杉醇给药系统的制备与抗癌活性
引用本文:冯霞,梁世乐,李晓锋,元英进.聚乙二醇支载紫杉醇给药系统的制备与抗癌活性[J].化工学报,2003,54(2):209-214.
作者姓名:冯霞  梁世乐  李晓锋  元英进
作者单位:天津大学化工学院制药工程系
基金项目:天津市导向性重大攻关项目 (No 983111811)
摘    要:利用紫杉醇分子中2′-羟基较高的反应活性,将紫杉醇连接到经氨基酸修饰后的水溶性聚乙二醇(PEG)分子上,制得了新型紫杉醇给药系统(DDS),测定了DDS的水溶性、紫杉醇含量及体外抗肿瘤活性.研究表明,此类系统水溶性良好(达紫杉醇的200~400倍),对乳腺癌MCF-7细胞和非小细胞肺癌PG细胞有很强的抑制作用,效果与紫杉醇相当,表明上述方法是解决紫杉醇水溶性及给药方式问题的可能方法之一.

关 键 词:紫杉醇  给药系统  水溶性  体外抗肿瘤活性  
文章编号:0438-1157(2003)02-0209-06
收稿时间:2001-6-27
修稿时间:2001年6月27日

PREPARATION AND ANTITUMOR EFFECT OF DRUG DELIVERY SYSTEM OF TAXOL CONJUGATED TO POLYETHYLENE GLYCOL
FENG Xia,LIANG Shile,LI Xiaofeng,YUAN Yingjin.PREPARATION AND ANTITUMOR EFFECT OF DRUG DELIVERY SYSTEM OF TAXOL CONJUGATED TO POLYETHYLENE GLYCOL[J].Journal of Chemical Industry and Engineering(China),2003,54(2):209-214.
Authors:FENG Xia  LIANG Shile  LI Xiaofeng  YUAN Yingjin
Abstract:A novel drug delivery system (DDS) of taxol was developed by linking taxol to a water-soluble polymer--polyethylene glycol (PEG) through amino acid spacer. Solubility of the DDS and content of taxol in them were dete rmined. Their antitumor activity were evaluated against two human tumor cell li nes: MCF-7 and PG. It was found that the DDS were more soluble in water than t axol and had similar cytotoxicity compared with the latter.In this way, a new k ind of DDS of taxol with improved water-solubility and potential antitumor acti vity was well established.
Keywords:taxol  drug delivery system(DDS)  water-soluble  in vitro  antitumor activity  
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