ENCAPSULATION, WITH HIGH-EFFICIENCY, OF RADIOACTIVE METAL-IONS IN LIPOSOMES
ENCAPSULATION, WITH HIGH-EFFICIENCY, OF RADIOACTIVE METAL-IONS IN LIPOSOMES
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DOI：
10.1016/0304-4165(82)90207-0
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发表时间：
1982-01-01
期刊：
影响因子：
--
通讯作者：
LUK, KFS
中科院分区：
文献类型：
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作者：
HWANG, KJ;MERRIAM, JE;LUK, KFS
放射性金属阳离子，如111 In 3+或67 Ga 3+，在脂质体的内部水室中的包封可以以约90%的效率实现。高比活度的阳离子到脂质体中的有效装载涉及111 In 3+或67 Ga 3+通过脂质双层转运到包封的强螯合物，如次氮基三乙酸，通过8-羟基喹啉，结合用于除去外部阳离子的有效阴离子交换树脂技术。8-羟基喹啉的浓度、脂质体和8-羟基喹啉-金属络合物的最终孵育混合物的pH以及装载孵育混合物中螯合剂的存在显著影响将阳离子装载到脂质体的效率。在pH 5 - 9的范围内，脂质体的内部水室的pH、脂质体的浓度、脂质体制备方法、脂质体的层状结构和脂质体的组成不影响装载效率。装载程序似乎不影响脂质体的大小和渗透性。有一个很好的协议，在组织分布的脂质体制备本负载方法和那些由传统的方法包封超声。脂质体包埋高比活度的~（67）Ga~（3+）或~（111）In~（3+），将有助于今后利用荧光成像和γ射线扰动角相关技术研究脂质体的体内动力学。
The encapsulation of radioactive metallic cations, such as 111In3+ or 67Ga3+, in the internal aqueous compartment of liposomes can be achieved with an efficiency of about 90%. The efficient loading of a high specific activity of cations into liposomes involves the transport of 111In3+ or 67Ga3+ through the lipid bilayer to an encapsulated strong chelate, such as nitrilotriacetic acid, by 8-hydroxyquinoline, in conjunction with an efficient anion-exchange resin technique for the removal of the external cations. The efficiency of loading cations to liposomes is affected markedly by the concentration of 8-hydroxyquinoline, the pH of the final incubation mixture of liposomes and the complex of 8-hydroxyquinoline-metal, and the presence of the chelating agents in the loading incubation mixture. The loading efficiency is not affected by the pH of the internal aqueous compartment of liposomes over a range of pH 5-9, the concentration of the liposomes, the method of liposomal preparation, the lamellar structure of the liposomes, and the composition of liposomes. The loading procedures do not appear to affect the size and the permeability of liposomes. There is a good agreement in the tissue distributions of the liposomes prepared by the present loading methods and those by the conventional method of encapsulation by sonication. Liposomes entrapping high specific activity of 67Ga3+ or 111In3+ will be useful for future studies of the in vivo kinetics of liposomes by the combined techniques of scintigraphic imaging and the gamma-ray perturbed angular correlation.