Wyniki wyszukiwania - Biblioteka Nauki

1

Preparation and evaluation of a [66Ga]gallium chitosan complex in fibrosarcoma bearing animal models

100%

Pourjavadi A. , Akhlaghi M. , Jalilian A. R.

|

tom Vol. 56, No. 1

35-40

EN

[66Ga]gallium chitosan complex was prepared with a high radiochemical purity (greater than 99%) in dilute acetic acid solution. The radiochemical purity of [66Ga]gallium chitosan complex was checked by using paper chromatography technique. The prepared complex solution was injected intratumoral to fibrosarcoma-bearing mice and the leakage of radioactivity from injection site was investigated. Approximately, 85.4% of the injected dose was retained in the injection site 54 h after injection and most of the leaked radioactivity was accumulated in the blood, liver (0.5%) and lung (6.5%).

2

Preparation, quality control and biodistribution studies of 165Dy-chitosan for radiosynovectomy

75%

Shirvani-Arani S. , Mahmoodabadi A. , Bahrami-Samani A. , Jalilian A. R. , Mazidi M. , Afarideh H. , Ghannadi-Maragheh M.

|

tom Vol. 56, No. 4

277-282

EN

The preparation of 165Dy-labeled chitosan for radiosynovectomy applications is described in this paper. 165Dy (T1/2 = 2.33 h) was prepared by irradiation of natural Dy(NO3)3 at a flux of 3.4 x 1013 neutrons/cm2.s for about 6 h. The irradiation resulted in the production of 11.1 GBq (300 mCi) of 165Dy activity. Emitting gamma ray (94.7 keV) and beta particles (Emax = 1.3 MeV, 83%) 165Dy decays to 165Ho. Eight hours after bombardment, the corresponding specific activity was 703 MBq/mg (19 mCi/mg). The irradiated target was dissolved in 0.1 N HCl solution. Radionuclidic purity was ascertained by high resolution gamma spectrometry. Chitosan solution was prepared in acetic acid solution (pH 3). The chitosan solution was labeled with 165Dy to prepare 165Dy-chitosan (165Dy-Chit) complex (labeling yield, greater than 99% and specific activity small tilde 3.7 TBq/mmol). In optimized conditions (pH 3, 35 mg/4 ml chitosan acidic solution, and 370 MBq of 165Dy) Chit was stable after 48 h. Bioevaluation of the prepared 165Dy-Chit was carried out by injecting 37 MBq (1 mCi, 50.100 mi1) directly into the knee joints of wild rats. Free 165Dy cation was also injected to study the effect of complex formation on the retention of radionuclide in the administered site. To study the consequence of radioactivity leakage from the administration site, a dilute sample of the complex was injected intravenously into the rats followed by biodistribution studies. It was observed that there was no significant extra-articular leakage of the injected activity over the study period of 24 h post-injection.

3

Biological evaluation of [18F]-nifedipine as a novel PET tracer for L-type calcium channel imaging

75%

Sadeghpour H. , Jalilian A. R. , Akhlaghi M. , Shafiee A. , Mirzaii M. , Miri R. , Saddadi F.

|

tom Vol. 53, No. 4

151-154

EN

Due to interesting role of dihydropyridines in cardiovascular diseases and drug resistance studies and lack of a fluorine-18 labeled imaging agent for L-type calcium channel studies, this study was designed. [18F]Dimethyl 2-(fluoromethyl)-6-methyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate 2 was prepared in no-carrier-added (n.c.a.) form from a starting brominated compound in one step at 80°C in Kryptofix2.2.2/[18F]. Compound 2 was administered to normal rats via their tail veins for preliminary biodistribution studies and the ID/g% of the labeled compound was determined up to 3 h post injections. Coincidence images were obtained in rats 5 to 120 min. Radiofluorination on bromo precursor gave a fluorinated compound in 95% radiochemical purity and a 8% yield shown by RTLC and HPLC. Biodistribution studies showed that the tracer is accumulated in the heart in the first few minutes, followed by metabolism resulting in very soluble 18F-containing metabolites eliminated through the urinary tract. In coincidence images, the target organ was shown to be the heart. Lung had high accumulation possibly due to the presence of Ca2+ channels and/or hydrolyzing enzymes showing a significant myocardial uptake at 120 min. The data demonstrates a significant agreement with the reported L-type calcium channels throughout the animal body. To our knowledge, this is the first example of 18F-DHPs in the literature.

4

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

75%

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

|

tom 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.

5

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

75%

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

|

2009

|

tom Vol. 54, No. 2

135-141

EN

[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.

6

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

75%

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

|

2009

|

tom 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.

7

Development of 153Sm-DTPA-rituximab for radioimmunotherapy

75%

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

|

2009

|

tom 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.

8

Preparation and biodistribution of 99mTc-IgG-HYNIC in normal rats

75%

Rajabifar S. , Akhlaghi M. , Jalilian A. R. , Bolourinovin F. , Maashkar B. , Talebimehrdar M. , Ghafouri M.

|

2009

|

tom Vol. 54, No. 4

279-284

EN

Human gamma globulin can be labeled by a direct or indirect method of radiotracer incorporated in a protein molecule. In this indirect method hydrazinonicotinic acid (HYNIC) is used which saves the structure and biological activity of the protein. Our goal was the efficient labeling of the human gamma globulin and evaluation of its biodistribution in different organs which can be used on experimentally induced infection causing inflammation. Immune globulin is mixed with s-hynic and IgG-hynic is developed using sidle A-lyzer and stored at –20°C which can be used at least for six months and then Sn-tricine kit is prepared which is used for 99mTc labeling. Efficiency of 99mTc-IgG-hynic labeling at pH 6.4 was very much dependent on ligand (hynic) and coligand (tricine) presence in the reaction mixture. Radiochemical purity was more than 90% in the kits prepared. Serum stability study showed no decomposition of 99mTc from the complex. The biodistribution studies showed the highest percentage ID/organ in the blood, liver and kidney, respectively. A human gamma globulin was successfully labeled through hynic to 99mTc by an indirect method with high radiochemical purity.