Journal of Cancer Research and Therapeutics

ORIGINAL ARTICLE
Year
: 2016  |  Volume : 12  |  Issue : 3  |  Page : 1117--1123

Samarium-153-(4-[((bis (phosphonomethyl)) carbamoyl) methyl]-7,10-bis (carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl) acetic acid: A novel agent for bone pain palliation therapy


Hassan Yousefnia1, Razieh Enayati2, Mohammad Hosntalab2, Samaneh Zolghadri1, Ali Bahrami-Samani1 
1 Nuclear Science and Technology Research Institute, Tehran, Iran
2 Faculty of Engineering, Science and Research Branch, Islamic Azad University, Tehran, Iran

Correspondence Address:
Hassan Yousefnia
Nuclear Science and Technology Research Institute, Tehran
Iran

Aim: Various phosphonate ligands labeled with β-emitting radionuclides have shown good efficacy for bone pain palliation. In this study, a new agent for bone pain palliation has been developed. Materials and Methods: Samarium-153-(4-[((bis(phosphonomethyl))carbamoyl)methyl]-7,10-bis (carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl) acetic acid (153Sm-BPAMD) complex was prepared using BPAMD ligand and samarium-153 chloride. The effect of various parameters on the labeling yield of 153Sm-BPAMD including ligand concentration, pH, temperature, and reaction time were studied. Production of 153Sm was performed at a research reactor using 152Sm (n, γ)153Sm nuclear reaction. The radiochemical purity of the radiolabeled complex was checked by instant thin layer chromatography. Stability studies of the complex in the final preparation and the presence of human serum were performed up to 48 h. Partition coefficient and hydroxyapatite (HA) binding of the complex were investigated and biodistribution studies using single photon emission computed tomography (SPECT) and scarification were performed after injection of the complex to wild-type mice. Results: 153Sm-BPAMD was prepared in a high radiochemical purity >98% and specific activity of 267 GBq/mmol at the optimal conditions. The complex demonstrated significant stability at the room temperature and in human serum at least for 48 h. HA binding assay demonstrated that at the amount of more than 5 mg, approximately, all radiolabeled complex was bind to HA. At the pH 7.4, log Po/w was − 1.86 ± 0.02. Both SPECT and scarification showed major accumulation of the labeled compound in the bone tissue. Conclusions: The results show that 153Sm-BPAMD has interesting characteristics as an agent for bone pain palliation, however, further biological studies in other mammals are still needed.


How to cite this article:
Yousefnia H, Enayati R, Hosntalab M, Zolghadri S, Bahrami-Samani A. Samarium-153-(4-[((bis (phosphonomethyl)) carbamoyl) methyl]-7,10-bis (carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl) acetic acid: A novel agent for bone pain palliation therapy.J Can Res Ther 2016;12:1117-1123


How to cite this URL:
Yousefnia H, Enayati R, Hosntalab M, Zolghadri S, Bahrami-Samani A. Samarium-153-(4-[((bis (phosphonomethyl)) carbamoyl) methyl]-7,10-bis (carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl) acetic acid: A novel agent for bone pain palliation therapy. J Can Res Ther [serial online] 2016 [cited 2017 Jan 16 ];12:1117-1123
Available from: http://www.cancerjournal.net/article.asp?issn=0973-1482;year=2016;volume=12;issue=3;spage=1117;epage=1123;aulast=Yousefnia;type=0