Preparation of 131I–betulinic acid and its biodistribution in murine model of hepatocellular tumor

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Abstract

The aim of this study was to examine the radioiodinating condition of betulinic acid and understand the possibility of 131I–betulinic acid (131I–BA) as a potential tumor radiotherapy agent through in vitro uptake and in vivo biodistribution studies 131I–BA was prepared by the reaction of betulinic acid with Na131I in the presence of hydrogen peroxide, and then purified by HPLC. The labeling yield was about 80%, and the radiochemical purity was greater than 95%. 131I–BA was found to be stable at 4 °C in saline containing 1% ethanol. In vitro studies showed that 131I–betulinic acid accumulated in the cancer cell lines (BEL-7402 and NCI-H446) in comparison with free 131I−. In vivo biodistribution study in KM mice bearing HepA tumor showed that 131I–BA stayed longer time in tumors than free 131I−. A significant differences were seen in tumor/muscle ratio at 4 h postinjection between 131I–BA and free 131I−. In vivo and in vitro studies showed the higher fraction of 131I–BA can be utilized for therapy and a higher dose will be delivered per targeting event. 131I–BA is a promising radiopharmaceutical in nuclear medicine, especially for hepatocellular tumor targeted radionuclide brachytherapy.

Keywords

131I–betulinic acid Radiolabeling Biodistribution 
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Notes

Acknowledgments

The authors thank the Health Ministry of Jiangsu Province and Wujiepin Medical Fund for the investigation support (No. H200735, RC2007096,320.6750.06116).

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Copyright information

© Akadémiai Kiadó, Budapest, Hungary 2010

Authors and Affiliations

  • Yu-Ping Xu
    • 1
  • Min Yang
    • 1
  • Dong-Hui Pan
    • 1
  • Li-Zhen Wang
    • 1
  1. 1.Jiangsu Institute of Nuclear Medicine; The Key Laboratory of Nuclear Medicine, Ministry of HealthWuxiChina

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