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Preparation and biological evaluation of [61Cu]bleomycin complex as a possible PET radiopharmaceutical in normal and fibrosarcoma-bearing animals

Jalilian A. R., Zandi H., Sardari D., Akhlaghi M., Kamali-Dehghan M., Shafaei K., Majdabadi A.

Nukleonika

2009

Vol. 54, No. 2

135-141

[61Cu]bleomycin ([61Cu]BLM) was prepared using [61Cu]CuCl2 produced via natZn(p,x)61Cu. [61Cu]BLM was prepared under optimized conditions (room temperature, 45 min, 0.1 mg bleomycin for 92.5–370 MBq 61CuCl2) with radiochemical purity over 98% shown by HPLC and RTLC. [61Cu]BLM was administered into normal and tumor bearing rodents up to 210 min followed by biodistribution and co-incidence imaging studies. A significant tumor/non tumor accumulation was observed either by animal sacrification or an imaging method. [61Cu]BLM can be a potential PET radiotracer for tumor imaging.

Development of 62Zn bleomycin as a possible PET tracer

Jalilian A., Fateh B., Ghergherehchi M., Karimian A., Moradkhani S., Kamali-Dehghan M., Tabeie F.

Nukleonika

2005

Vol. 50, nr 4

143-148

Abstract Bleomycin (BLM), labeled with radioisotopes, is widely used in therapy and diagnosis. In this study, BLM was labeled with 62Zn for oncologic PET studies. The complex was obtained at pH = 2 in saline at 90°C in 25 min. Radio-TLC showed an overall radiochemical yield of 95 97% (radiochemical purity > 97%). Stability of complex was checked in vitro in mice and human plasma/urine. Preliminary in vivo studies were performed to determine complex stability and distribution of 62Zn BLM in normal and fibrosarcoma-bearing mice. 62Zn BLM accumulated significantly in induced fibrosarcoma tumors in mice according to biodistribution/imaging studies. 62Zn BLM can be used in PET oncology studies due to its suitable physicochemical properties as a diagnostic complex in vitro and in vivo. Further studies should be performed for evaluation of the complex behavior in larger mammals.

Development of 111In-DTPA-human polyclonal antibody complex for long-term inflammation/infection detection

Jalilian A., Rowshanfarzad P., Shafaii K., Kamali-Dehghan M., Moafian J., Akhlaghi M., Babaii M., Rajabifar S., Mirzaii M.

Nukleonika

2005

Vol. 50, nr 3

91-96

Human polyclonal antibody (HIgG) was successively labeled with 111In-indium chloride after residulation with freshly prepared cyclic DTPA-dianhydride. The best results of the conjugation were obtained by the addition of solid DTPA-dianhydride (0.1 0.3 mg) to 100 mi l of the HIgG solution (0.2 0.4 mg/ml) at pH = 6 in phosphate buffer media at 25°C with continuous stirring for 30 min. Radio-thin-layer chromatography showed an overall radiochemical yield of 96 99% at optimized conditions (specific activity = 300 500 MBq/mg, radiochemical purity >98%). The final isotonic 111In-DTPA-HIgG complex was checked by radio-TLC to ensure the formation of only one species followed by filtration through a 0.22 mi filter. Preliminary long-term in vivo studies in turpentine-oil induced inflammation in rat model was performed to determine late complex distribution of the radioimmunoconjugate. The target/skin and target/ blood ratios were 27 and 51 after 24 h, and 23 and 51 after 110 h, showing a high selectivity of the radiopharmaceutical for inflammatory lesions.