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Preparation, quality control and biodistribution studies of [61Cu]-oxinate for PET tumor imaging

Jalilian A. R., Zolghadri S., Faghihi R., Yousefnia H., Garousi J., Shafaii K., Bolourinovin F.

Nukleonika

2009

Vol. 54, No. 3

175-179

Targeting apoptosis is an interesting issue in molecular imaging and various modalities have been presented. However, recent experiences in nuclear pharmacy demonstrated the application of small tracer molecules is more desired. This work was conducted for production of a radiolabeled copper complex, i.e. 61Cu-oxinate as a potential PET tracer for apoptosis imaging in oncology. Cu-61 was prepared by natural zinc target irradiation with 22 MeV protons (150 miA) via the natZn(p, xn)61Cu nuclear reaction with a yield of 3.33 mCi/miAh. In order to obtain the best labeling method, optimization reactions were performed for pH, temperature and concentration followed by solid phase extraction. Biodistribution of the tracer was studied in wild-type and fibrosarcoma bearing mice. Under the optimized conditions, radio-thin-layer chromatography (RTLC) and HPLC showed radiochemical purities of 99.99% and 97% respectively (with a minimum specific activity of 16 Ci/mM). Biodistribution of the tracer in fibrosarcoma bearing mice demonstrated a significant tumor uptake after 3 h. Tumor:blood and tumor:muscle ratios were 2.0 and 6.0 after 3 h, respectively.

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.

Preparation of [61Cu]DTPA complex as a possible PET tracer

Jalilian A., Rowshanfarzad P., Sabet M., Kamalidehghan M.

Nukleonika

2006

Vol. 51, nr 2

111-117

Copper-61 (T1/2 = 3.33 h) produced via the 64Zn(p,alfa)61Cu nuclear reaction, using a natural zinc target, was separated from the irradiated target material by two ion exchange chromatography steps and was used for the preparation of [61Cu]-diethylenetriaminepentacetate ([61Cu]DTPA) using freshly-prepared DTPA cyclic dianhydride. An electroplated natural zinc layer on a gold-coated copper backing was irradiated with 22 MeV protons (22 12 MeV on the target, 180 miA irradiation, 3.2 h, final activity 220 GBq of 61Cu2+, RCY > 95%, radionuclidic purity > 99%, 60Cu as the only radionuclidic impurity; T1/2 = 23.7 min). Colorimetric methods showed that traces of chemical impurities in the product were below the accepted limits. The solution of [61Cu]DTPA was prepared with a radiochemical yield of more than 80% starting with 61CuOAc ligand at room temperature after 30 min. RTLC showed the radiochemical purity of more than 99%. The specific activity obtained was about 9.1 TBq/mmol. The tracer was shown to be stable in the final product and in the presence of human serum at 37°C up to 3 h.