Synthesis and biological assessment of folate-accepted developer 99mTc-DTPA-folate-polymer
Synthesis and biological assessment of folate-accepted developer 99mTc-DTPA-folate-polymer
复制标题
叶酸可接受的显色剂 99mTc-DTPA-叶酸聚合物的合成和生物学评估
DOI：
10.1016/j.bmcl.2016.03.084
复制
发表时间：
2016-05-15
影响因子：
2.7
通讯作者：
Jiang, Mengjun
中科院分区：
文献类型：
--
作者：
Chen, Fei;Shao, Kejing;Jiang, Mengjun
A novel cancer-targetable folate-poly(2-hydroxyethyl methacrylate) (PFDH) copolymer containing DTPA segment was prepared by conventional chemical synthesis and labeled with Tc-99m subsequently. The Tc-99m-labled PFDH could be produced easily with high radiochemical yield of 91% and radiochemical purity of 95%. The LogP octanol-water value for the Tc-99m-labled PFDH was -2.19 and the radiotracer was stable in phosphate-buffered saline and human serum for 2 h (>95% in PBS or similar to 90% in human serum). To investigate Tc-99m-labled PFDH tumor targeting, the in vitro and in vivo stability, cell uptake, in vivo biodistribution, and SPECT imaging were evaluated, respectively. These preliminary results strongly suggest that the novel folate conjugated dendrimer maybe developed to be potential for delivery of therapeutic radionuclides. (C) 2016 Elsevier Ltd. All rights reserved.
