title: An Optimized Protocol for the Efficient Radiolabeling of Gold Nanoparticles by Using a 125I-labeled Azide Prosthetic Group.
abstract: Here, we demonstrate a detailed protocol for the radiosynthesis of a125I-labeled azide prosthetic group and its application to the efficient radiolabeling of DBCO-group-functionalized gold nanoparticles using a copper-free click reaction. Radioiodination of the stannylated precursor (2) was carried out by using [125I]NaI and chloramine T as an oxidant at room temperature for 15 min. After HPLC purification of the crude product, the purified125I-labeled azide (1) was obtained with high radiochemical yield (75 ± 10%, n = 8) and excellent radiochemical purity (>99%). For the synthesis of radiolabeled 13-nm-sized gold nanoparticles, the DBCO-functionalized gold nanoparticles (3) were prepared by using a thiolated polyethylene glycol polymer. A copper-free click reaction between 1 and 3 gave the125I-labeled gold nanoparticles (4) with more than 95% of radiochemical yield as determined by radio-thin-layer chromatography (radio-TLC). These results clearly indicate that the present radiolabeling method using a strain-promoted copper-free click reaction will be useful for the efficient and convenient radiolabeling of DBCO-group-containing nanomaterials.
authors: Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute; Department of Radiation Biotechnology and Applied Radioisotope Science, University of Science and Technology; jeonj@kaeri.re.kr.
authors: Jongho
authors: J
authors: Jeon
authors: Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute.
authors: Ha Eun
authors: HE
authors: Shim
authors: Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute; Department of Radiation Biotechnology and Applied Radioisotope Science, University of Science and Technology.
authors: Sajid
authors: S
authors: Mushtaq
authors: Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute.
authors: Mi Hee
authors: MH
authors: Choi
authors: Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute; Department of Radiation Biotechnology and Applied Radioisotope Science, University of Science and Technology.
authors: Sang Hyun
authors: SH
authors: Park
authors: Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute.
authors: Dae Seong
authors: DS
authors: Choi
authors: Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute; Department of Radiation Biotechnology and Applied Radioisotope Science, University of Science and Technology; jangbs@kaeri.re.kr.
authors: Beom-Su
authors: BS
authors: Jang
mesh_terms: D001386:Azides; D002855:Chromatography, Thin Layer; D057930:Click Chemistry; D006046:Gold; D007457:Iodine Radioisotopes; D053758:Nanoparticles
chemical_list: D001386:Azides; D007457:Iodine Radioisotopes; D006046:Gold