Synthesis and biological assessment of folate-accepted developer ^99mTc-DTPA-folate-polymer

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• 作者：Fei Chen^a ; Kejing Shao^a ; Bao Zhu^a ; ^{zhubao_999@126.com" class="auth_mail" title="E-mail the corresponding author} ; Mengjun Jiang^b ; ^{jmj16888@126.com" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Synthesis ; Polymer ; Folate ; 99mTc ; Cancer imaging
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：15 May 2016
• 年：2016
• 卷：26
• 期：10
• 页码：2547-2550
• 全文大小：493 K

文摘

A novel cancer-targetable folate-poly(2-hydroxyethyl methacrylate) (PFDH) copolymer containing DTPA segment was prepared by conventional chemical synthesis and labeled with ^99mTc subsequently. The ^99mTc-labled PFDH could be produced easily with high radiochemical yield of 91% and radiochemical purity of 95%. The Log P octanol–water value for the ^99mTc-labled PFDH was −2.19 and the radiotracer was stable in phosphate-buffered saline and human serum for 2 h (>95% in PBS or ∼90% in human serum). To investigate ^99mTc-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.