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Preparation and quality control of lutetium-177 bleomycin as a possible therapeutic agent

Yousefnia H., Jalilian A. R., Zolghadri S., Bahrami-Samani A., Shirvani-Arani S., Ghannadi-Maragheh M.

Nukleonika

2010

Vol. 55, No. 3

285-291

Due to interesting therapeutic properties of 177Lu and antineoblastic antibiotic, bleomycin (BLM), 177Lu-bleomycin (177Lu-BLM) was developed as a possible therapeutic compound. Lu-177 of 2.6-3 GBq/mg specific activity was obtained by irradiation of a natural Lu2O3 sample with a thermal neutron flux of 4 × 1013 nźcm-2źs-1. The product was converted into chloride form which was further used for labeling of BLM. In optimized conditions a radiochemical purity of 98% was obtained for 177Lu-BLM shown by instant thin-layer chromatography (ITLC) (specific activity, 740 GBq/mmole). Biodistribution studies of Lu-177 chloride and 177Lu-BLM were performed in wild-type rats. The accumulation of the radiolabeled compound in lungs, liver and spleen demonstrates a pattern similar to the other radiolabeled bleomycins. Lu-BLM is a possible therapeutic agent in human malignancies and the efficacy of the compound should be tested in various tumor-bearing models.

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.