[show abstract][hide abstract] ABSTRACT: Due to the antitumor activity of Gallium MAL complex, as well as recent findings on new targeted biomolecules in malignant cells through this complex, the development of radiolabeled gallium complex for future imaging studies was targeted. Ga-67 labeled 3-hydroxy-2-methyl-4H-pyran-4-onate (Ga-67 MAL) was prepared using freshly prepared Ga-67 chloride and 3-hydroxy-2-methyl-4H-pyran-4-onate in a sodium salt form in 25 min at 40° C. The stability of the complex was checked in final formulation and human serum for 24 h followed by the administration in Swiss mice for biodistribution studies. The complex was prepared in high radiochemical purity (> 97% ITLC, > 98% HPLC) and specific activity of 13-14 GBq/mmol and was stable in the presence of serum for 48 h. The partition coefficient was calculated for the compound (log p = 0.40). A detailed comparative pharmacokinetic study was performed for Ga-67 cation and Ga-67-MAL. The complex is more rapidly washed out from the circulation through kidneys and liver compared to Ga-67 cation and can be an interesting tumor imaging agent due to the fact that the cold compound is undergoing clinical trials as a safe and potential therapeutic agent for cancer.
Iranian journal of pharmaceutical research (IJPR) 01/2012; 11(3):755-62. · 0.54 Impact Factor
[show abstract][hide abstract] ABSTRACT: In this study, superparamagnetic iron oxide nanoparticles (SPION) embedded by folic acid (SPION-folate) were prepared by a
modified co-precipitation method. The structure, size, morphology, magnetic property and relaxivity of the SPION-folate were
characterized systematically by means of XRD, VSM, HRSEM and TEM and the interaction between folate and iron oxide (Fe3O4) was characterized by FT-IR. The particle size was shown to be ≈5–10 nm. To ensure biocompatibility, the interaction of these
SPION with mouse connective tissue cells (adhesive) was investigated using an MTT assay. Consequently, gallium-67 labeled
nanoparticles ([67Ga]-SPION-folate) were prepared using 67Ga with a high labeling efficiency (over 96%, RTLC method) and they also showed an excellent stability at room temperature
for at least 2 days and were evaluated for their biodistribution in normal rats up to 24 h compared with free Ga3+ cation and [67Ga]-SPION biodistribution. The biodistribution of the tracer among 3 other folate tracers were compared, showing lower liver
uptake and higher blood circulation after 24 h leading to better bioavailability. The bone:muscle, kidney:muscle, lung:muscle,
stomach:muscle ratios were 9.3, 9.32, 7.6 and 5.83 respectively. The developed folate-containing nano-system can be an interesting
folate receptor tracer, capable of better cell membrane permeability while possessing paramagnetic properties for thermotherapy.
Journal of Radioanalytical and Nuclear Chemistry 01/2011; 287(1):119-127. · 1.47 Impact Factor
[show abstract][hide abstract] ABSTRACT: Abstract
Aim Due to the interesting pharmacologic properties of
porphyrins, the idea of developing a possible tumor
imaging agent using PET by incorporating 68Ga into a
suitable porphyrin ligand was investigated.
Methods 68Ga-labeled 5,10,15,20-tetrakis(pentafluoro-13
phenyl) porphyrin (68Ga-TFPP) was prepared using freshly
eluted [68Ga]GaCl3 obtained from a 68Ge/68Ga generator
developed in-house and 5,10,15,20-tetrakis(pentafluorophenyl)
porphyrin (H2TFPP) for 60 min at 100°C.
Results The complex was prepared with high radiochemical
purity (>99% ITLC, >99% HPLC, specific activity: 13–14
GBq/mmol). Stability of the complex was checked in the final
formulation and in human serum for 5 h. The partition
coefficient was calculated for the compound (log P = 0.62).
The biodistribution of the labeled compound in vital organs
of Swiss mice bearing fibrosarcoma tumors was studied
using scarification studies and SPECT imaging up to 1 h.
The complex was mostly washed out from the circulation
through kidneys and liver. The tumor-to-muscle ratio 1
h post injection was 5.13.
Conclusion The radiolabeled porphyrin complex demonstrated
potential for further imaging studies in other tumor
[show abstract][hide abstract] ABSTRACT: The goal of this research was to investigate the potential of newly synthesized gold complex trichloro(2,4,6-trimethylpyridine)Au(III) as an anticancer agent. The gold(III) complex was synthesized and grafted on nanoporous silica, MCM-41, to produce AuCl(3)@PF-MCM- 41 (AuCl(3) grafted on pyridine-functionalized MCM-41). The toxicity of trichloro(2,4,6- trimethylpyridine)Au(III) and AuCl(3)@PF-MCM-41 in Saccharomyces cerevisiae (as a model system) was studied. The gold(III) complex showed a mid cytotoxic effect on yeast viability. Using the drug delivery system, nanoporous MCM-41, the gold(III) complex became a strong inhibitor for growth of yeast cells at a very low concentration. Furthermore, the animal tests revealed a high uptake of AuCl(3)@PF-MCM-41 in tumor cells. The stability of the compound was confirmed in human serum.
International Journal of Nanomedicine 01/2011; 6:3251-7. · 3.46 Impact Factor
[show abstract][hide abstract] ABSTRACT: Introduction: Due to the interesting pharmacological properties of radiolabeled metal oxine derivatives such as cell internalization, tumor avidity and antiproteosome activity, 111 In-tris[8-Hydroxy-2-methylquinoline] (111 In-HMQ) was developed in this study. Methods: 111 In-HMQ was prepared using 111 InCl 3 and 8-Hydroxy-2-methylquinoline (HMQ) for 60 min at 100C (radiochemical purity: >99% ITLC, >99% HPLC, specific activity: 13-14 GBq/mmol). Stability of the complex was checked in final formulation and in the presence of human serum for 48 h. The partition coefficient was calculated for the compound (log P=0.68). Results: The biodistribution of the labeled compound in vital organs of wild-type rats was studied using scarification studies and SPECT up to 24 h. A detailed comparative pharmacokinetic study for 111 In cation and 111 In-HMQ are performed up to 24h. Conclusion: The complex is mostly cleaned from the circulation by kidneys and is a compound rapidly washing from the circulation. The biodistribution of the complex in tumor models is on-going.
Iranian Journal of Nuclear Medicine 01/2011; 19(2):20-27.
[show abstract][hide abstract] ABSTRACT: A new aluminium alkoxide, Al(OCH2CH2OCH2CH2OCH3)3, with donor-functionalized group was prepared and characterized by elemental analysis, mass spectrometry, and 1H, 13C and 27Al NMR spectroscopy. The prepared aluminium alkoxide was used as a precursor for the synthesis of alumina by the sol–gel processing. The physiochemical properties of alumina that were obtained from hydrolysis of Al(OCH2CH2OCH2CH2OCH3)3 were investigated and compared with that of alumina synthesized from aluminium 2-butoxide. Utilizing Al(OCH2CH2OCH2CH2OCH3)3 as a precursor in sol–gel processing resulted in formation of alumina with significantly lower surface area, smaller pore volume, and pore size in comparison with alumina obtained from aluminium 2-butoxide. A novel morphology was observed for the alumina prepared from aluminium alkoxide with donor-functionalized group.
Materials Letters - MATER LETT. 01/2010; 64(4):503-505.
[show abstract][hide abstract] ABSTRACT: Tl-201 has potential in the preparation of radiolabelled compounds similar to its homologues, like In-111 and radiogallium. In this paper, recently prepared [(201)Tl](III) vancomycin complex ([(201)Tl](III)VAN) has been evaluated for its biological properties.
[(201)Tl](III)VAN was prepared according to the optimized conditions followed by biodistribution studies in normal rats for up to 52 h. The Staphylococcus aurous specific binding was checked in vitro. The complex was finally injected to normal rats. Tracer SPECT images were obtained in normal animals and compared to those of (67)Ga-citrate.
Freshly-prepared [(201)Tl](III)VAN batches (radiochemical yield > 99%, radiochemical purity > 98%, specific activity approximately 1.2 Ci/mmol) showed a similar biodistribution to that of unlabeled vancomycin. The microorganism binding ratios were 3 and 9 for tracer (201)Tl(3+) and tracer (201)Tl(III)DTPA, respectively, suggesting the preservation of the tracer bioactivity. As a nonspecific cell penetrating tracer, [(201)Tl](III)DTPA was used.
Nuclear medicine review. Central & Eastern Europe: journal of Bulgarian, Czech, Macedonian, Polish, Romanian, Russian, Slovak, Yugoslav societies of nuclear medicine and Ukrainian Society of Radiology 02/2008; 11(1):1-4.
[show abstract][hide abstract] ABSTRACT: [61Cu]-labeled pyruvaldehyde-bis(N-4-methylthiosemicarbazone) (61Cu-PTSM), a promising agent made for imaging blood perfusion, was produced via the natZn(p, x)61Cu nuclear reaction in a 30 MeV cyclotron, and separated by a two-step column chromatography method developed in our laboratory using a cation and an anion exchange resin. After 150 μA irradiation for 76 min, about 6.006 Ci of 61Cu2+ was obtained with a radiochemical separation yield of 95% and a radionuclidic purity of 99%. 61Cu-PTSM was prepared using an optimized method with in-house synthesized PTSM ligand for radiolabeling following quality control procedures using RTLC and HPLC. The tracer is mostly incorporated in heart, kidneys and brain compared to free copper cation as a control. These are in agreement with former reports. In conclusion, [61Cu]-PTSM was prepared at the radiopharmaceutical scales with high quality and is a potential PET tracer in the perfusion study of the heart, kidney, brain and tumors.
Nuclear Science and Techniques 01/2008; 19(3):159-164. · 0.09 Impact Factor
[show abstract][hide abstract] ABSTRACT: Co-55 (t1/2=17.53 h) was produced by 150 μA irradiation of a natural nickei target using 15 MeV protons. It was separated from the irradiated target material by two ion exchange chromatography steps with a radiochemical yield of >95% and was used for the preparation of [55Co]vancomycin ([55Co]VAN). Optimization studies were performed using Co-57 due to its longer half-life. Cobalt-57 (t1/2=271.79 d) was produced by irradiation of a natural nickel target with 150 μA current of 22 MeV protons. The 57Co was separated from the irradiated target material using a no-carrier-added method with a radiochemical yield of >97%. Both products were controlled for radionuclide and chemical purity. The solutions of [55Co]VAN were prepared (radiochemical yield >80%) starting with 55Co acetate and vancomycin at room temperature after 30 min. A precise solid phrase extraction (SPE) method was developed using Si Sep-Pak in order to purify/reconstitute the final formulation for animal studies. [55Co]VAN showed a radiochemical purity of more than 99%. The resultant specific activity was about 1.15 TBq/mmol. It is proved that the tracer is stable in the final product and in presence of human serum at 37°C up to 24 h. Biodistribution study of [55Co]VAN in normal rats was undertaken for up to 72 h.
Nuclear Science and Techniques - NUCL SCI TECH. 01/2008; 19(6):347-353.
[show abstract][hide abstract] ABSTRACT: 61 Cu]-N-(2-hydroxyacetophenone)glycinate ([ 61 Cu]NHAG) was prepared using in house-made NHAG ligand and [ 61 Cu]CuCl 2 produced via the nat Zn(p,x) 61 Cu (180μA proton irradiation, 22MeV, 3.2h) and purified by a ion chromatography method. [ 61 Cu]NHAG radiochemical purity was >98% and >99.9% by RTLC and HPLC methods respectively after purification by SPE. [ 61 Cu]NHAG was administered into normal and tumor bearing mice followed by biodistribution studies up to 180 minutes. The best tumor accumulation was observed by animal sacrification after 120 min (tumor/muscle and tumor/blood ratios were 25.6 and 3.4 respectively). [ 61 Cu]NHAG is a potential PET radiotracer for tumor imaging.