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A. R. Jalilian, M. Akhlaghi, B. Shirazi, R. Aboudzadeh, Gholamreza Raisali, M. Salouti, M. Babaii

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

Keywords: 201Tl(III)-complexation, Bleomycin, Biodistribution, SPECT, Fibrosarcoma

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 (T_1/2=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.

Radiochimica Acta, Oldenbourg Wissenschaftsverlag

Print ISSN: 0033-8230
Volume: 94, 08/2006
Pages: 453 - 459

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