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Development of a radiolabeled glucagon compound for imaging

Jalilian A. R., Jouiaei M., Doroudi A. R., Bolourinovin F., Garousi J.

Nukleonika

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2010

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Vol. 55, No. 2

219-224

EN

In order to develop a possible Ga-labeled glucagon (GCG) compound for imaging studies, biosynthetic glucagon (GCG) was labeled with [67Ga]-gallium chloride after conjugation with freshly prepared diethylenetriaminepentaacetic acid dianhydride (ccDTPA). After solid phase purification of the radiolabeled hormone, high performance liquid chromatography (HPLC) and instant thin-layer chromatography (ITLC) showed a radiochemical purity around 95 per cent in optimized conditions (specific activity = 296–370 GBq/mM; labeling efficiency 85 per cent). Preliminary in vivo studies (IDźg–1 per cent) in male wild-type rats showed heart:muscle, liver:muscle, lung:muscle and stomach:muscle ratios to be 5.53, 2.9, 7.56, 3.69, 3.2 (in 5 min), respectively while after 2 h liver:blood, lung:blood and spleen:blood ratios were 14.21, 16.86 and 7.8, respectively. The data suggests 5 min post injection, the tracer is accumulated in GCGR rich tissues which is in agreement with biodistribution studies and reported GCG receptors (GCGRs). The results of the present study can possibly offer a candidate for non-invasive imaging of glucagon receptor related diseased and malignancies such as glucagonoma.

2

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

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2009

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Vol. 54, No. 3

175-179

EN

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.

3

Development of 153Sm-DTPA-rituximab for radioimmunotherapy

Bahrami-Samani A., Ghannadi-Maragheh M., Jalilian A. R., Yousefnia H., Garousi J., Moradkhani S.

Nukleonika

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2009

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Vol. 54, No. 4

271-277

EN

Combining beta-particle effect with therapeutic properties of anti-CD20 monoclonal antibody in lymphomas, Mabthera™ (rituximab) was targeted in this study. The antibody was labeled with 153Sm-samarium chloride (185 MBq) after conjugation with freshly prepared ccDTPA. Conjugated-rituximab was obtained by the addition of 1 ml of a rituximab pharmaceutical solution (5 mg/ml, in phosphate buffer, pH = 7.8) to a glass tube precoated with freshly prepared ccDTPA (0.01–0.1 mg) at 25 degrees centigrade. Sm-153 chloride was obtained by a thermal neutron flux (5 × 1013 nźcm–2źs–1) of an enriched 152Sm2O3 sample, dissolved in acidic media. Radiolabeling was performed in one hour by the addition of DTPA-rituximab conjugate at room temperature. Radiochemical purity of 96% (ITLC) and 98% (HPLC) were obtained for the final radioimmunoconjugate (specific activity = 120 TBq/mmol). The final isotonic 153Sm-rituximab complex was checked by gel electrophoresis for protein integrity retention. Biodistribution studies in normal rats were performed to determine radioimmunoconjugate distribution up to 24 h. SPECT images were also obtained using 103 keV photons up to 48 h.

4

Preparation and biodistribution of [67Ga]-insulin for SPECT purposes

Jalilian A. R., Garousi J., Gholami E., Akhlaghi M., Bolourinovin, Rajabifar S.

Nukleonika

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2007

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Vol. 52, nr 4

145-151

EN

Human recombinant insulin was successively labeled with [67Ga]-gallium chloride after conjugation with freshly prepared cyclic DTPA-dianhydride (ccDTPA). The best results of the conjugation were obtained by the addition of 0.5 ml of an insulin pharmaceutical solution (5 mg/ml, in phosphate buffer, pH = 8) to a glass tube precoated with DTPA-dianhydride (0.01 mg) at 25°C with continuous mild stirring for 30 min. Radiothin-layer chromatography (RTLC), instant thin-layer chromatography (ITLC) and high-performance liquid chromatography (HPLC) showed overall radiochemical purity higher than 96% in optimized conditions (specific activity = 300 500 MBq/mg, labeling efficiency 77%). Preliminary in vivo studies with normal rats were performed to determine the biodistribution of the radiotracer up to 110 h. They showed a high liver uptake of the tracer which is consistent with other reported radiolabeled insulins.