^(99)Tc^m-MAG_3-Lys-mPEG的制备及其在小鼠体内的分布

Preparation and Biodistribution of ^(99)Tc^m-MAG_3-Lys-mPEG

以mPEG-5000、Fmoc-Lysine和MAG3为原料,经过五步反应合成了载体MAG3-Lys-mPEG;对其进行99Tcm标记后,进一步研究了标记物的体外稳定性及其在小鼠体内的生物分布。结果表明,99Tcm-MAG3-Lys-mPEG的标记率>98%;标记物在体外有很好的稳定性,在生理盐水中放置24 h时,放化纯度>91%;在血清中温浴16.5 h时放化纯度仍>92%;标记物在小鼠体内的血液清除较快,在肾脏中的摄取最高,标记物主要经肾脏通过尿液排出体外。mPEG有可能用作反义核酸的有效载体。

Starting with mPEG-5000, Fmoc-Lysine, and mercaptoacetyltriglycine （MAG3）,the carrier MAGa-Lys-mPEG is synthesized through five steps, which carrier is labeled by ^99Tc^m with labeling efficiency 〉98%.^99Tc^m-MAG3-Lys-mPEG shows high stability in vitro.The radiochemical purity keeps up 〉91 % and 〉92% after incubation in saline for 24 h and in bovine serum for 16.5 h, respectively. The biodistribution in mice indicates that ^99Tc^m-MAG3-Lys-mPEG is quickly cleared from blood, and excreted mainly through the urinary systemr. There is the highest uptake in kidneys. It is expected that mPEG may be used as an effective ASODN carrier.