Abstract: Liposome is an effective nuclide delivery agent for neutron capture therapy. In this paper liposomes 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.

Key words: neutron capture therapy, liposome, gadolinium complex, tumor cell

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，Gd-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Gd-EDTA作为钆中子俘获治疗药物的可能性。

关键词: 中子俘获治疗, 脂质体, 钆配合物, 癌细胞