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脂质体作为钆中子俘获治疗肿瘤药物载体的跨膜动力学及机理研究

Kinetics and Mechanism Study of Across-Membrane Transport of Liposome as a Carrier for Gadolinium Neutron Capture Therapy

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【作者】 邹娟任春李铁军陈丽蓉王祥云刘元方

【Author】 ZOU Juan PEN Chun LI Tiejun CHEN Lirong WANG Xiangyun LIU Yuanfang (Division of applied Chemistry , Department of Technical Physics , Peking University, Beijing , 100871)

【机构】 北京大学技术物理系应用化学专业

【摘要】 制备和表征了包埋Gd-EDTA的脂质体,测定了pH,离子强度,缓冲液组成及温度对Gd- EDTA脂质体的影响,比较了Gd-EDTA脂质体和Gd-EDTA被肿瘤细胞摄入的动力学曲线。结果表明,Cd-EDTA脂质体在37℃和生理条件下最稳定,肿瘤细胞摄入Gd-EDTA脂质体速率是Gd- EDTA的8倍,而释放Gd的速率,Gd-EDTA脂质体远远低于Gd—EDTA,这些结果提供了脂质体包埋Cd-EDTA作为钆中子俘获治疗药物的可能性。

【Abstract】 Liposome is an effective nuclide delivery agent for neutron capture therapy. In this paper lipo-somes containing encapsulated gadolinium complex (LGd) were prepared and characterized. The influence of formulation factors such as pH, ionic strength ,buffer, and storage time upon the stability of liposomes was investigated. The uptake rate constant and its concentration dependence of LGd in tumor cells were compared in vitro with that of Gd complex itself. The results indicate that the uptake rate of LGd in tumor cells increases to eight times as much as that of Gd-EDTA, but the release rate of Gd from tumor cells containing LGd is remarkably lower than that from the tumor cells containing Gd-EDTA. The results reveal that LGd would be a potential drug for neutron capture therapy of cancer,

【基金】 国家科委“九·五”攀登B资助项目
  • 【会议录名称】 脂质体及紫杉醇脂质体学术论文集
  • 【会议时间】2005-11
  • 【分类号】R94
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