153Sm-DTPA-PNIPAAm的制备及其在荷瘤鼠体内的分布

    Preparation and Biodistribution of 153Sm-DTPA-PNIPAAm in TumorBearing Mice

    • 摘要: 合成了带双功能偶联剂二乙三胺五醋酸(DTPA)的热敏高分子DTPA-PNIPAAm,它保持了聚(N-异丙基丙烯酰胺)(PNIPAAm)的热敏性。探讨了153Sm-DTPA-PNIPAAm的制备条件和体外稳定性,经皮下瘤内注入后标记物在荷瘤鼠体内的分布。结果表明,室温下153Sm-DTPA-PNIPAAm的最佳标记条件为,pH=7~9,配体质量为20~25 mg,反应时间大于20 min;最高标记率为93.4%;标记物的体外稳定性较高,76 h内标记物的放化纯度保持在96.5%以上;皮下瘤内注入后,标记物主要滞留在注入点肿瘤组织内,3 d时其滞留率为(83.2±9.7)%。

       

      Abstract: A thermo-sensitive poly(N-isopropylacrylamide) (PNIPAAm) with terminal group DTPA was designed and synthesized, and the DTPA-PNIPAAm showed similar low critical solution temperature (LCST) to that of PNIPAAm. The preparation conditions of 153Sm-DTPA-PNIPAAm, stability in vitroand biodistribution after intratumoral injection in tumorbearing mice were investigated. The experimental results of preparation investigation show that it is better to prepare 153Sm-DTPA-PNIPAAm at pH=7-9 with 20-25 mg of DTPA-PNIPAAm and the reaction time more than 20 min. The labeling efficiency under the best reaction conditions is 93.4%. The labeled complex is stable in vitroand the radiochemical purity remains 96.5% after 76 h. After intratumoral injection, (83.2±9.7)% of the total radioactivity is kept at injected position after 72 h.

       

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