<sup>177</sup>Lu-DTPA-BIS-BIOTIN的制备及正常鼠体内生物分布

¹⁷⁷Lu-DTPA-BIS-BIOTIN的制备及正常鼠体内生物分布

摘要: 研究了DTPA-BIS-BIOTIN的¹⁷⁷Lu标记方法，优化了标记条件，并进行了标记物在正常小鼠体内分布实验。在最佳标记条件下（DTPA-BIS-BIOTIN 25 μg，标记介质pH=4.5，80℃反应20 min），¹⁷⁷Lu-DTPA-BIS-BIOTIN标记率大于99.0%,室温下放置96 h，标记物体外稳定性良好。正常小鼠体内分布实验结果表明,¹⁷⁷Lu-DTPA-BIS-BIOTIN在血液中清除快，主要浓集于肝、脾和肾,经肾脏排泄。本研究为进一步采用¹⁷⁷Lu-DTPA-BIS-BIOTIN进行肿瘤预定位显像及治疗研究提供了实验基础。

Abstract: The labeling method for ¹⁷⁷Lu-DTPA-BIS-BIOTIN was established, and the biodistribution of ¹⁷⁷Lu-DTPA-BIS-BIOTIN in normal mice was carried out as well. Under the optimal experimental condition (DTPA-BIS-BIOTIN 25 μg，pH=4.5 reacting at 80℃ for 20 min), the labeling yield of ¹⁷⁷Lu-DTPA-BIS-BIOTIN is more than 99.0%. ¹⁷⁷Lu-DTPA-BIS-BIOTIN shows pretty good in vitro stability. The biodistribution of ¹⁷⁷Lu-DTPA-BIS-BIOTIN in normal mice shows a rapid blood clearance. The uptake of ¹⁷⁷Lu-DTPA-BIS-BIOTIN is mainly accumulated in liver, spleen and kidney. ¹⁷⁷Lu-DTPA-BIS-BIOTIN is excreted by kidney. The results provide the basis for further study on ¹⁷⁷Lu-DTPA-BIS-BIOTIN used in pretargeted radioimage and radiotherapy of cancer.