Search Results
Abstract
The reaction of 99mTc of different oxidation states (+7, +4) with 2-thiouracil and 5-nitrobarbituric acid have been studied at different temperatures, pH and concentrations. The reaction mixtures have been analyzed at different times using thin layer chromatography (TLC) and a radio detector to show the peaks at the plates. 99mTc is obtained from the Mo generators with oxidation state (+7). The use of SnCl2 as a reducing agent gave 99mTc with oxidation state (+4). It is very difficult to separate the complexes formed from the reactions in very small concentration. The percentage of 99mTc and its oxidation state involved in the complexes can be determined. The labeling efficiencies (percentage of complex) in the reaction of 99mTc+7 with 5-nitro-barbituric-acid increases mostly at pH 10. Both oxidation states of 99mTc(+7, +4) can be detected at pH’s 4 and 10, but at pH 4, the reduced form 99mTCO2, is more pronounced. At pH 7 no complexes were detected and most of 99mTc remains as 99mTCO4 − . By increasing the ligand concentration, the labeling efficiencies of the complex increases. For the reaction of 99mTc of oxidation states (+4, +7) with 2-thiouracil at different temperatures and analytical times it is concluded that several complexes with different Rf values were observed in equilibrium and most of these complexes were unstable.
Abstract
Meropenem was successfully radiolabeled with 99mTc in high labeling yield (92 ± 2%) and stability (~6 h). 99mTc–meropenem showed high accumulation in tumor hypoxic tissue (4.193% injected dose/g organ). 99mTc–meropenem showed high ability to differentiate the tumor tissue from inflamed or infected tissues in different mice models as its T/NT ratio ~4 in case of tumor mice model while T/NT ratio ~1 in case of inflamed mice model. So, 99mTc–meropenem showed high selectivity in comparison with FDG-PET and 99mTc-nitroimidazole analogues. Thus, 99mTc–meropenem could be used as a selective potential imaging agent for diagnosis of tumor hypoxia.
Abstract
Pyrroloquinoline quinone (PQQ), an essential nutrient, antioxidant, redox modulator and nerve growth factor found in a class of enzymes called quinoproteins, was labeled with 99mTc by using stannous fluoride (SnF2) method. Radiolabeling qualification, quality control and characterization of 99mTc-PQQ and its biodistribution studies in mice were performed and discussed. Effects of pH values, temperature, time and reducing agents concentration on the radiolabeling yield were investigated. The quality control procedure of 99mTc-PQQ was determined by thin layer chromatography (TLC), radio high-performance liquid chromatography (RHPLC) and paper electrophoresis methods. The average radiolabeling yield was 94 ± 1% under optimum conditions of 0.99 mg of PQQ, 30 μg of SnF2, 0.5 mg of ethylenediaminetetraacetic acid disodium salt (EDTA-2Na) and 18.5 MBq of Na99mTcO4 at pH 6 and 25 °C with a response volume of 1 ± 0.1 mL. 99mTc-PQQ was stable and anionic. Lipid–water partition coefficient of 99mTc-PQQ was −1.49 ± 0.16. The pharmacokinetics parameters of 99mTc-PQQ were t 1/2α = 18.16 min, t 1/2β = 100.45 min, K 12 = 0.013 min−1, K 21 = 0.017 min−1, K e = 0.016 min−1, AUC (area under the curve) = 1040.78 ID% g−1 min and CL (plasma clearance) = 0.096 mL min−1. The dual-exponential equation was Y = 10.88e−0.038t + 5.21e−0.0069t . The biodistribution of 99mTc-PQQ was studied in ICR (Institute for Cancer Research 7701 Burhelme Are., Fox Chase, Philadelphia, PA 1911 USA) mice. In vitro autoradiographic studies clearly showed that the 99mTc-PQQ radioactivity accumulated predominantly in the hippocampus and cortex, which had a high density of N-methyl-d-aspartate Receptor (NMDAR). The enrichment can be blocked by NMDAR redox modulatory site antagonists-ebselen (EB) and 99mTc-PQQ is therefore a promising candidate for the molecular imaging of NMDAR. To date, however, there have been no studies characterizing 99mTc-PQQ.
Abstract
Bombesin (BNN)-like peptides have very high binding affinity for the gastrin-releasing peptide (GRP) receptor. The goal of the current study was to optimize the labeling conditions of a new 99mTc-radiolabeled BNN-like peptide based on the bifunctional chelating ligand HYNIC using different co-ligands (EDDA and tricine). The radiolabeling conditions (pH, amount of co-ligand, amount of stannous chloride, temperature and reaction time) for newly-formed 99mTc-tricine-HYNIC-Q-Litorin and 99mTc-EDDA-HYNIC-Q-Litorin were optimized and evaluated by RHPLC and RTLC. Radiochemical yields for 99mTc-tricine-HYNIC-Q-Litorin and 99mTc-EDDA-HYNIC-Q-Litorin were 98.0 ± 1.7 and 97.5 ± 2.5%, respectively. When EDDA was used as co-ligand, the labeling of 99mTc-EDDA-HYNIC-Q-Litorin was optimal in the following reaction mixture: HYNIC-peptide: EDDA: 10 μg/5 mg, pH 3, SnCl2 concentration: 12 μg/0.1 mL, reaction temperature: 100 °C, reaction time: 15 min. Besides, the optimum conditions were HYNIC-peptide:tricine: 10 μg/50 mg, pH 5, SnCl2 concentration: 12 μg/0.1 mL, reaction temperature: 100 °C, reaction time: 15 min for preparing 99mTc-tricine-HYNIC-Q-Litorin. The manufactured 99mTc-HYNIC-Q-Litorin conjugates may offer new possibilities for imaging cancer cells expressing bombesin receptors.
Abstract
Labelling of meso-2,3-dimercaptosuccinic acid (DMSA) with technetium-99m was reinvestigated. Dependence of the 99mTc-DMSA complex formation on the molar ratio of DMSA:reducing agent (SnCl2·2H2O) and pH was studied. Five different types of 99mTc-DMSA complexes were determined. Especially three different complexes were established in the clinically used and prepared DMSA kit labelled with 99mTc under alkaline condition. This radiopharmaceutical is used as imaging agent of the primary medullary carcinoma in the thyroid gland and different metastasis types. The existence of all complexes was observed by paper chromatography, paper electrophoresis and high performance liquid chromatography.
Abstract
99mTc–rufloxacin (99mTc–RUN) complex was prepared by reaction of different amounts of reduced sodium pertechnetate with different amount of Rufloxacin (RUN) antibiotic for the in vivo scintigraphic localization of the Staphylococcus aureus (S. aureus) infectious foci in Male Wister Rats (MWR) model. The 99mTc–RUN complex was radiochemically and biologically characterized in terms of radiochemical stability in saline, serum, in vitro binding with S. aureus and biodistribution in artificially infected with S. aureus MWR. The 99mTc–RUN complex showed stability more than 90% up to 240 min in normal saline with a maximum stability value of 98.10 ± 0.18% at 30 min after reconstitution. At 37 °C the complex showed in vitro permanence in serum up to 16 h with 13.90% side products during incubation. The 99mTc–RUN complex showed saturated in vitro binding with S. aureus at different intervals with a maximum uptake value of 71.50%. Infected to normal muscle, infected to inflamed and inflamed to normal muscles ratios were approximately 6.04, 4.31 and 1.40. Based on the stability of the complex in saline, serum, in vitro binding with S. aureus and biodistribution results, the 99mTc–RUN complex is recommended for in vivo scintigraphic localization of the S. aureus in vivo infectious foci in human.
Abstract
Metronidazole (MTNZ) is an antiprotozoa drug, could be labeled with the 99mTc. MTZL could be used as an ideal vehicle to deliver radioactive decay energy of 99mTc to the sites of tumor, thus facilitate tumor imaging. The process of labeling was done using tin chloride as reducing agent. The optimum conditions required to label 25 μg MTZL were 100 μg stannous chloride, 30 min reaction time, room temperature at pH 7–9 using 0.5 M phosphate buffer. The radiochemical purity of the labeled compound, at the above conditions, was determined using paper chromatography. The yield was about 93%. About 2.5 × l06 of Ehrlich Ascites Carcinoma (EAC) was injected intrapritoneally (i.p) to produce ascites and intramuscularly (i.m) in the right thigh to produce solid tumor in female mice. Biodistribution studies were carried out by injecting solution of 99mTc-MTZL in normal and tumor bearing mice. The uptake in ascites was over 5% of the injected dose per gram tissue body weight, at 4 h post injection and above 4% in solid tumor. These data revealed localization of the tracer in the tumor tissues with high percentage sufficient to use 99 mTc MTZL as promising tool for diagnosis of tumor.
Abstract
Cefotaxime, a cephalosporin antibiotic, used to treat bacterial infections was investigated to label with 99mTc. Labeling was performed using sodium dithionite as a reducing agent at 100 °C for 10 min and radiochemical analysis involved ITLC and HPLC methods. The stability of labeled antibiotic was checked in the presence of human serum at 37 °C up to 24 h. The maximum radiolabeling yield was 92 ± 2%. Bacterial binding assay was performed with S. aureus and the in vivo distribution was studied in mice. Images showed minimal accumulation in non-target tissues, with an average target/non-target ratio of 2.89 ± 0.58.
Abstract
Shikonin was isolated from Ratanjot pigment then the obtained shikonin was well characterized. This study is aimed to optimize radiolabeling yield of shikonin with 99mTc with respect to factors that affect the reaction conditions such as shikonin amount, SnCl2·2H2O amount, reaction time and pH of the reaction mixture. In vitro stability of the radiolabeled complex was checked and it was found to be stable for up to 6 h. Biodistribution studies showed that, 99mTc–shikonin accumulate in tumor sites with higher T/NT than other currently available 99mTc(CO)3-VIP, 99mTc–nitroimidazole analogues and 99mTc–polyamine analogues indicating that shikonin deliver 99mTc to the tumor sites with a percentage sufficient for imaging and can overcome many drawbacks of other radiopharmaceuticals used for tumor imaging.
Abstract
Glycyl-l-proline (Gly-l-Pro) is the main degradation product of collagen and is a good diagnostic tool in various pathological conditions. The aim of this work was to prepare dipeptide Gly-l-Pro labeled with 99mTc. Complex preparation was carried out under alkaline reaction conditions and its stability was assessed 10 and 120 min after preparation. The formation of two types of complex compounds was observed. High-performance liquid chromatography, paper electrophoresis, paper chromatography and thin layer chromatography were employed to monitor the formation of different complexes. Molecular modeling (semi-empirical method) was used to design their structure and composition. First complex cI with formula [TcO(Gly-l-Pro)]−1 is unstable. After 120 min cI is completely transformed to complex cII with formula Tc(Gly-l-Pro)3.
