title: Synthesis and in vivo evaluation of 99m Tc-Transferrin conjugate for detection of inflamed site.
abstract: Transferrin is one of acute phase reactants in inflamed lesion. Expression of transferrin receptor is increased in activated macrophage during inflammation process. Conjugates of target ligand with novel water-soluble chitosan for fast excretion of background radioactivity have been shown to be selectively taken up via the target molecules. In this study, radiolabeled 99m Tc-Transferrin conjugate was synthesized and evaluated its efficacy in vivo as a targeted agent for the rapid detection of inflamed lesion that expresses relatively high level of transferrin receptors. Transferrin was conjugated with HYNIC-chitosan and radiolabeled with 99m Tc. The biodistribution and scintigraphic images with the 99m Tc-HYNIC-chitosan-Transferrin conjugate (99m Tc-Tfc) were studied in a murine infection model in which the infection was induced with Escherichia coli (2 x 10(6) colonies). The %ID/g was as follows: 1.612 +/- 0.098, 2.473 +/- 0.202 and 2.617 +/- 0.646% at 30, 120 min and 6 h after injection, respectively. Gamma camera imaging rapidly visualized the infection/inflammation lesion, with the lesion-to-background ratio improving with time up to 5.68 +/- 0.48. 99m Tc-Tfc scintigraphy allows rapid and good imaging of an inflamed lesion.
authors.affiliation: Department of Nuclear Medicine, Research Institute of Clinical Medicine, Institute for Medical Sciences, Chonbuk National University Medical School and Hospital, Jeonju, Chonbuk, South Korea.
authors.forename: Eun-Mi
authors.initials: EM
authors.lastname: Kim
authors.forename: Hwan-Jeong
authors.initials: HJ
authors.lastname: Jeong
authors.forename: Se-Lim
authors.initials: SL
authors.lastname: Kim
authors.forename: Chang-Moon
authors.initials: CM
authors.lastname: Lee
authors.forename: Dong Wook
authors.initials: DW
authors.lastname: Kim
authors.forename: Seok Tae
authors.initials: ST
authors.lastname: Lim
authors.forename: Myung Hee
authors.initials: MH
authors.lastname: Sohn
mesh_terms: D000818:Animals; D015153:Blotting, Western; D002460:Cell Line; D005260:Female; D007249:Inflammation / Q000000981:diagnostic imaging*; D051379:Mice; D008807:Mice, Inbred BALB C; D008856:Microscopy, Fluorescence; D015609:Organotechnetium Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D011877:Radionuclide Imaging; D014018:Tissue Distribution; D014168:Transferrin / Q000138:chemical synthesis* / Q000493:pharmacokinetics
chemical_list: D015609:Organotechnetium Compounds; D014168:Transferrin