Synthesis and biological assessment of folate-accepted developer (99m)Tc-DTPA-folate-polymer.

Bioorg Med Chem Lett

Department of Clinical Laboratory Science, Nanjing Medical University, Affiliated Wuxi People's Hospital, Wuxi, Jiangsu 214023, PR China. Electronic address:

Published: May 2016

AI Article Synopsis

  • A novel copolymer, PFDH, was developed which targets cancer cells and is labeled with (99m)Tc, achieving high radiochemical yield and purity.
  • The (99m)Tc-labeled PFDH exhibited great stability in both phosphate-buffered saline and human serum for a period of 2 hours.
  • Preliminary studies indicate that this folate-conjugated dendrimer could be a promising method for delivering therapeutic radionuclides directly to tumors.

Article Abstract

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

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Source
http://dx.doi.org/10.1016/j.bmcl.2016.03.084DOI Listing

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