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表面带活性羧基的新型长循环脂质体的制备和组织分布研究(英文)

Preparation and Biodistribution In Mice of Long-circulating Liposomeswith Active Carboxylic Terminals

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【作者】 张宇锋张朔侯新朴谢蜀生王琦

【Author】 Zhang Yufeng 1 , Zhang Shuo 1 , Hou Xinpu 1 ** 1. School of Pharmaceutical Sciences, Beijing Medical University, Beijing 100083; Xie Shusheng 2 , 2. Department of Immunopharmacology, College of Basic Medical Science, Beijing Medical University, Beijing 10

【机构】 北京医科大学药学院物理药学研究室!北京 100083北京医科大学基础医学院免疫药理研究室!北京 100083中国原子能研究院氚标记室!北京 102412

【摘要】 合成和纯化了一个带末端羧基的新的磷脂酰乙醇胺的聚乙二醇衍生物3/4DPPE-PEG3000-COOH。 将这个化合物掺入脂质体后,脂质体在网状内皮系统(肝、脾)的聚集减少,在血中的循环时间明显延长,并表现为一级对数线性消除。脂质体表面的活性羧基可以和其它活性分子反应,这可能为脂质体带来新的功能。

【Abstract】 A new PE-PEG derivative with an active carboxylic terminal, DPPE-PEG3000-COOH, was synthesized and purified. Its incorporation into small unilamellar liposomes composed of egg phosphatidylcholine and cholesterol conferred the liposomes prolonged circulation in blood and reduced accumulation in the RES, as the traditional methoxy-PEG derivatives of PE displayed. With the active carboxylic groups on the surface, DPPE-PEG3000- COOH liposomes can be linked with some active molecules, which provide liposomes with special functions.

【基金】 Supported by National Natural Science Foundation of China !(39770879) and State Laboratory of Intelligent Technology and Systems
  • 【文献出处】 Journal of Chinese Pharmaceutical Sciences ,中国药学(英文版) , 编辑部邮箱 ,2000年03期
  • 【分类号】R944
  • 【被引频次】2
  • 【下载频次】168
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