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[201Tl](III)-bleomycin for tumor imaging

  • A. R. Jalilian , M. Akhlaghi , B. Shirazi , R. Aboudzadeh , Gholamreza Raisali , M. Salouti and M. Babaii
Published/Copyright: September 25, 2009

Summary

Due to interesting physical properties and wide availability of thallium-201 as a SPECT radionuclide, the idea of incorporation of this nuclide into biologically active compounds was targeted. Thallium-201 (T1/2 = 3.04 d) in Tl+ form was converted to Tl3+ cation in presence of O3 in 6 M HCl controlled by RTLC/gel electrophoresis methods. The final evaporated activity was reacted with bleomycin in normal saline to yield [201Tl]BLM at room temperature after 0.5 h (radiochemical yield > 99%) followed by HPLC analysis. The studies showed that thallic ion is mostly incorporated into bleomycin A2 while other species in the pharmaceutical sample almost remain unlabeled. Radiochemical purity of more than 99% was obtained using RTLC, HPLC with specific activity of about 7 Ci/mmol. The stability of the tracer was checked in the final product in presence of human serum at 37 °C up to 3 d. The tracer accumulated in tumors of fibrosarcoma-bearing mice after 72 h.

Received: 2006-1-24
Accepted: 2006-5-3
Published Online: 2009-9-25
Published in Print: 2006-8-1

© Oldenbourg Wissenschaftsverlag

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