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Development of a New FR-Targeting Agent 99mTc-HYNFA with Improved Imaging Contrast and Comparison of Multimerization and/or PEGylation Strategies for Radio-Folate Modification

This study aims to develop a new folate receptor (FR)-targeting agent for SPECT imaging with improved contrast and evaluate the modification strategies of multimerization and/or PEGylation in the development of new radio-folates. A series of novel folate derivatives have been synthesized and radiolabeled with 99mTc using tricine and TPPTS as coligands. To better investigate their pharmacokinetics, cell uptake, biodistribution, and microSPECT/CT imaging were evaluated. Four radioligands displayed high KB cell uptake after incubation for 2 and 4 h. Presaturated with excess folic acid (FA) resulted in a significant blocking effect in KB cells, indicating specificity of these radioligands toward FR. Biodistribution and microSPECT imaging studies in KB tumor-bearing mice showed that the folate conjugate 99mTc-HYNFA with poly(ethylene glycol) (PEG) and triazole linkage displayed the highest tumor uptake (16.30 ± 2.01 %ID/g at 2 h p.i. and 14.9 ± 0.62 %ID/g at 4 h p.i. in mice biodistribution) and best imaging c...

Authors:   Zhide Guo; Linyi You; Changrong Shi; Manli Song; Mengna Gao; Duo Xu; Chenyu Peng; Rongqiang Zhuang; Ting Liu; Xinhui Su; Jin Du; Xianzhong Zhang
Journal:   Molecular Pharmaceutics
Year:   2017
DOI:   10.1021/acs.molpharmaceut.7b00536
Publication date:   12-Oct-2017
Facts, background information, dossiers
  • pharmacokinetics
  • folic acid
  • ethylene glycol
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