Synthesis And Biological Assessment Of Folate-Accepted Developer Tc-99m-Dtpa-Folate-Polymer

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.