title: Synthesis and biological assessment of folate-accepted developer (99m)Tc-DTPA-folate-polymer.
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.
authors.affiliation: Department of Nuclear Medicine, Nanjing Medical University, Affiliated Wuxi People's Hospital, Wuxi, Jiangsu 214023, PR China.
authors.forename: Fei
authors.initials: F
authors.lastname: Chen
authors.affiliation: Department of Nuclear Medicine, Nanjing Medical University, Affiliated Wuxi People's Hospital, Wuxi, Jiangsu 214023, PR China.
authors.forename: Kejing
authors.initials: K
authors.lastname: Shao
authors.affiliation: Department of Nuclear Medicine, Nanjing Medical University, Affiliated Wuxi People's Hospital, Wuxi, Jiangsu 214023, PR China. Electronic address: zhubao_999@126.com.
authors.forename: Bao
authors.initials: B
authors.lastname: Zhu
authors.affiliation: Department of Clinical Laboratory Science, Nanjing Medical University, Affiliated Wuxi People's Hospital, Wuxi, Jiangsu 214023, PR China. Electronic address: jmj16888@126.com.
authors.forename: Mengjun
authors.initials: M
authors.lastname: Jiang
mesh_terms: D000818:Animals; D060326:Chemistry Techniques, Synthetic; D004355:Drug Stability; D005260:Female; D005492:Folic Acid / Q000737:chemistry*; D056945:Hep G2 Cells; D006801:Humans; D008819:Mice, Nude; D011102:Polyhydroxyethyl Methacrylate / Q000737:chemistry; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics*; D016284:Technetium Tc 99m Pentetate / Q000737:chemistry* / Q000493:pharmacokinetics; D014018:Tissue Distribution; D015899:Tomography, Emission-Computed, Single-Photon / Q000379:methods
chemical_list: D019275:Radiopharmaceuticals; D011102:Polyhydroxyethyl Methacrylate; D005492:Folic Acid; D016284:Technetium Tc 99m Pentetate
keywords: (99m)Tc; Cancer imaging; Folate; Polymer; Synthesis