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177Lu–labeled micro liposomes as a potential radiosynoviorthesis therapeutic agent
International Journal of Pharmaceutics ( IF 5.8 ) Pub Date : 2021-09-17 , DOI: 10.1016/j.ijpharm.2021.121106
Đorđe Cvjetinović 1 , Drina Janković 2 , Zorana Milanović 2 , Marija Mirković 2 , Jelena Petrović 2 , Željko Prijović 2 , Emiliya Poghosyan 3 , Sanja Vranješ-Đurić 2
Affiliation  

Micro–sized multivesicular liposomes were prepared, radiolabeled with 177Lu, and tested in vitro and in vivo to evaluate the potential of 177Lu–labeled micro liposomes in radiosynoviorthesis (RSO) therapy. A standard reverse–phase procedure of liposome preparation with a lipid mixture of DPPC: CHOL (80:20%) was used for the synthesis. TEM and fluorescence microscopy imaging were performed to determine the size, shape, and structure of the prepared liposomes. Both measurements are in good agreement while TEM micrographs additionally indicate to a large multivesicular inner structure of prepared liposomes. A simple and straightforward procedure was used for liposome radiolabeling with 177Lu, a well–known and commonly used radionuclide in radiotherapy with favorable properties, that can be exploited in RSO therapy. Radiolabeled 177Lu–liposomes were tested in vitro for stability and then injected into the knee joints of Wistar rats where liposome in vivo behavior was followed up to 30 days post injection. Results from both ex vivo biodistribution and in vivo imaging studies presented a high stability and retention (>94 %ID) of 177Lu–micro liposomes in the synovial liquid for the entire observation period. Leakage of free 177Lu or 177Lu–liposomes from the synovial fluid has not been detected, indicating to a possible application of 177Lu–liposomes in radiosynoviorthesis (RSO) therapy.



中文翻译:

177Lu 标记的微脂质体作为潜在的放射滑膜治疗剂

制备微型多囊脂质体,用177 Lu 进行放射性标记,并进行体外体内测试以评估177 Lu 标记的微型脂质体在放射滑膜术 (RSO) 治疗中的潜力。脂质体制备的标准反相程序与 DPPC: CHOL (80:20%) 的脂质混合物用于合成。进行 TEM 和荧光显微镜成像以确定制备的脂质体的大小、形状和结构。两种测量结果都非常一致,而 TEM 显微照片还表明制备的脂质体具有大的多囊泡内部结构。一个简单而直接的程序用于脂质体放射性标记与177Lu 是放射治疗中众所周知且常用的放射性核素,具有良好的特性,可用于 RSO 治疗。放射性标记的177 Lu-脂质体在体外进行稳定性测试然后注射到 Wistar 大鼠的膝关节中,注射后 30 天跟踪脂质体的体内行为。从两个结果离体生物分布和体内成像研究提出了很高的稳定性和保留的(> 94%ID)177路微脂质体在整个观察期内滑膜液。游离177 Lu或177泄漏尚未检测到滑液中的 Lu-脂质体,这表明177 Lu-脂质体可能在放射滑膜术(RSO) 治疗中得到应用。

更新日期:2021-09-22
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