Ogihara-Umeda I, Sasaki T, Nishigori H
Faculty of Pharmaceutical Sciences, Teikyo University, Kanagawa, Japan.
Int J Rad Appl Instrum B. 1992 Oct;19(7):753-7. doi: 10.1016/0883-2897(92)90136-m.
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.
将各种放射性核素 - 配体复合物包裹于脂质体中，并研究它们在肿瘤中的蓄积情况。观察到每种复合物以脂质体包裹形式存在时，肿瘤蓄积量均增加。然而，尽管所有放射性核素均采用相似的脂质体制剂递送，但不同放射性核素的蓄积水平有所不同。脂质体在循环中保持完整，但最终在肿瘤、肝脏和脾脏中会发生降解。因此，这表明脂质体包裹的放射性核素在肿瘤中的蓄积不仅取决于脂质体自身的体内行为，还取决于核素 - 配体复合物从脂质体释放后的特性。正确选择用于包裹在脂质体中的放射性核素和配体将能够实现优良的肿瘤成像剂。
