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

Yu-Ping Xu; Min Yang; Dong-Hui Pan; Li-Zhen Wang

doi:10.1007/s10967-010-0925-6

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Journal of Radioanalytical and Nuclear Chemistry

Volume/Issue:: Volume 288: Issue 1

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

Authors:

Yu-Ping Xu

Yu-Ping Xu Jiangsu Institute of Nuclear Medicine; The Key Laboratory of Nuclear Medicine, Ministry of Health, 20 Qianrong Road, 214063 Wuxi, China

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Min Yang

Min Yang Jiangsu Institute of Nuclear Medicine; The Key Laboratory of Nuclear Medicine, Ministry of Health, 20 Qianrong Road, 214063 Wuxi, China

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Dong-Hui Pan

Dong-Hui Pan Jiangsu Institute of Nuclear Medicine; The Key Laboratory of Nuclear Medicine, Ministry of Health, 20 Qianrong Road, 214063 Wuxi, China

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, and

Li-Zhen Wang

Li-Zhen Wang Jiangsu Institute of Nuclear Medicine; The Key Laboratory of Nuclear Medicine, Ministry of Health, 20 Qianrong Road, 214063 Wuxi, China

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Pages:: 157–161

Online Publication Date:: 23 Dec 2010

Publication Date:: 01 Apr 2011

Article Category:: Research Article

DOI:: https://doi.org/10.1007/s10967-010-0925-6

Keywords:: 131I–betulinic acid; Radiolabeling; Biodistribution

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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.

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Journal of Radioanalytical and Nuclear Chemistry

Print ISSN:: 0236-5731

Online ISSN:: 1588-2780

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Journal of Radionalytical and Nuclear Chemistry
Language	English
Size	A4
Year of Foundation	1968
Volumes per Year	1
Issues per Year	12
Founder	Akadémiai Kiadó
Founder's Address	H-1117 Budapest, Hungary 1516 Budapest, PO Box 245.
Publisher	Akadémiai Kiadó Springer Nature Switzerland AG
Publisher's Address	H-1117 Budapest, Hungary 1516 Budapest, PO Box 245. CH-6330 Cham, Switzerland Gewerbestrasse 11.
Responsible Publisher	Chief Executive Officer, Akadémiai Kiadó
ISSN	0236-5731 (Print)
ISSN	1588-2780 (Online)