Development of a liposome-encapsulated radionuclide with preferential tumor accumulation—the choice of radionuclide and chelating ligand

Izumi Ogihara-Umeda, Toru Sasaki, Hideo Nishigori
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引用次数: 17

Abstract

Various radionuclide-ligand complexes were encapsulated in liposomes and their accumulations in tumors were studied. Increased tumor accumulation was observed with every complex in the liposome-encapsulated form. However, different accumulation levels were registered for the various radionuclides even though they were all delivered using a similar liposome formulation. Though the liposomes remained intact in the circulation, they were degraded in the tumor, liver and spleen eventually. Thus, this suggests that tumor accumulation of liposome-encapsulated radionuclides is dependent on not only the in vivo behavior of the liposomes themselves, but also the characteristics of nuclide—ligand complexes after their release from liposomes. A correct choice of radionuclides and ligands for encapsulation in liposomes would enable excellent tumor-imaging agents to be achieved.

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具有肿瘤优先蓄积性的放射性核素脂质体的研制——放射性核素与螯合配体的选择
研究了各种放射性核素-配体复合物在脂质体中的包封及其在肿瘤中的积累。每一种脂质体包封形式的复合物都观察到肿瘤堆积增加。然而,各种放射性核素的积累水平不同,即使它们都是使用类似的脂质体配方递送的。尽管脂质体在循环中保持完整,但它们最终在肿瘤、肝脏和脾脏中被降解。因此,这表明放射性核素脂质体在肿瘤中的蓄积不仅取决于脂质体本身的体内行为,还取决于它们从脂质体释放后核素-配体复合物的特性。正确选择放射性核素和配体包封在脂质体中,可以获得优异的肿瘤显像剂。
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