대한방사성의약품학회지 (Journal of Radiopharmaceuticals and Molecular Probes)

  • 제7권2호
  • /
  • Pages.79-84
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  • 2021
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  • 2384-1583(pISSN)
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  • 2508-3848(eISSN)
대한방사성의약품학회 (Korean Society of Radiopharmaceuticals and Molecular Probes)
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Synthesis of a PEGylated tracer for radioiodination and evaluation of potential in tumor targeting

  • Abhinav Bhise (Department of Molecular Medicine, Brain Korea 21 Four KNU Convergence Educational Program of Biomedical Sciences for Creative Future Talents, School of Medicine, Kyungpook National University) ;
  • Sushil K Dwivedi (Department of Molecular Medicine, Brain Korea 21 Four KNU Convergence Educational Program of Biomedical Sciences for Creative Future Talents, School of Medicine, Kyungpook National University) ;
  • Kiwoong Lee (Department of Molecular Medicine, Brain Korea 21 Four KNU Convergence Educational Program of Biomedical Sciences for Creative Future Talents, School of Medicine, Kyungpook National University) ;
  • Jeong Eun Lim (Department of Molecular Medicine, Brain Korea 21 Four KNU Convergence Educational Program of Biomedical Sciences for Creative Future Talents, School of Medicine, Kyungpook National University) ;
  • Subramani Rajkumar (Department of Molecular Medicine, Brain Korea 21 Four KNU Convergence Educational Program of Biomedical Sciences for Creative Future Talents, School of Medicine, Kyungpook National University) ;
  • Woonghee Lee (Department of Molecular Medicine, Brain Korea 21 Four KNU Convergence Educational Program of Biomedical Sciences for Creative Future Talents, School of Medicine, Kyungpook National University) ;
  • Seong Hwan Cho (Department of Molecular Medicine, Brain Korea 21 Four KNU Convergence Educational Program of Biomedical Sciences for Creative Future Talents, School of Medicine, Kyungpook National University) ;
  • Jeongsoo Yoo (Department of Molecular Medicine, Brain Korea 21 Four KNU Convergence Educational Program of Biomedical Sciences for Creative Future Talents, School of Medicine, Kyungpook National University)
  • 투고 : 2021.11.16
  • 심사 : 2021.12.28
  • 발행 : 2021.12.30
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초록

Radiopharmaceuticals are important for tumor diagnosis and therapy. To deliver a radiotracer at the desired target excluding non-targeted tissues is difficult The development of a targeted tracer that has a good clearance profile while maintaining high biostability and biocompatibility is key to optimizing its biodistribution and transport across biological barriers. Improving the hydrophilicity of radiotracers by PEGylation can reduce serum binding, allowing the tracer to circulate without retention and reducing its affinity for non-targeted tissues. In this study, we synthesized a new benzamido tracer (SnBz-PEG36) with the introduction of a low molecular weight polyethylene glycol unit (PEG36, ~2,100 Da). The tumor targeting efficiency and biodistribution of [131I]-Bz-PEG36 or radiotracer-loaded liposomes were evaluated after their administration to normal mice or mouse tumor models including CT26 (xenograft) and 4T1 (xenograft and orthotopic). Most of the radiotracer was cleared out rapidly (1-24 h post-administration) through the kidney and there was little tumor uptake.

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과제정보

This work was supported by an R&D program through the National Research Foundation of Korea funded by the Ministry of Science, ICT & Future Planning (Nos.2019H1D3A1A01102643 and 2020R1C1C1008442).

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