Factors affecting eluation characteristics of sorption generators of technetium-99m

The influence of the adsorbed mass of molybdenum on the width of eluation profiles of generators and the patterns of molybdenum distribution in the amount of chromatographic columns by scanning them on the germanium-gallium detector using collimating device are studied. The boundary conditions under which the maximum value of {99m}Tc yield from generators Y[e]=1 are defined. After scanning the columns, it was found out that the degree of filling the columns with molybdenum Q and the value of its maximum adsorption depend naturally on the total weight of the adsorbed mass. In order to achieve the condition Y[e]=1 the value of Q should be at least 85%

Radiopharmaceuticals for SPECT Cancer Detection

The purpose of the study was to assess the efficacy of single photon emission computed tomography (SPECT) with {199}Tl and {99}mTc-MIBI in the detection of breast, laryngeal and hypopharyngeal cancers. A total of 220 patients were included into the study: 120 patients with breast lesions (100 patients with breast cancer and 20 patients with benign breast tumors) and 100 patients with laryngeal/hypopharyngeal diseases (80 patients with laryngeal/hypopharyngeal cancer and 20 patients with benign laryngeal/hypopharyngeal lesions). No abnormal {199}Tl uptake was seen in all patients with benign breast and laryngeal lesions, indicating a 100% specificity of {199}Tl SPECT. In the breast cancer patients, the increased {199}Tl uptake in the breast was visualized in 94.8% patients, {99m}Tc-MIBI-in 93.4% patients. The increased {199}Tl uptake in axillary lymph nodes was detected in 60% patients, and {99m}Tc-MIBI-in 93.1% patients. In patients with laryngeal/hypopharyngeal cancer, the sensitivity of SPECT with {199}Tl and {99m}Tc-MIBI was 95%. The {199}Tl SPECT sensitivity in identification of regional lymph node metastases in the patients with laryngeal/hypopharyngeal cancer was 75% and the {99m}Tc-MIBI SPECT sensitivity was 17%. The data obtained showed that SPECT with {199}Tl and {99m}Tc-MIBI can be used as one of the additional imaging methods in detection of tumors

Development new radiopharmaceutical based on 5-thio-d- glucose labeled technetium-99m

The article considers the obtaining and possibility of using 5-thio-D-glucose labeled technetium-99m for the diagnosis of malignant tumors by single photon emission computed tomography. The analysis of the level of international developments of radiopharmaceuticals based on derivatives of glucose has been carried out. Also the article provides information on of using experimental batches of lyophilisate on the basis of 5-thio-D-glucose for preliminary biomedical testing on the mice

Development and Study of {99m}Tc-1-Thio-D-glucose for Visualization of Malignant Tumors

The preclinical studies of {99m}Tc-1-Thio-D-glucose, a new tumor-seeking agent based on technetium-99mlabeled glucose derivative, were conducted, and the feasibility of using this radiopharmaceutical for tumor visualization was studied. The preclinical studies were carried out strictly in accordance with the local legislation and were regulated by the generally accepted research standards. {99m}Tc-1-Thio-D-glucose was found to have optimal pharmacokinetic and physico-chemical properties for diagnostic imaging and was proved to belong to the low-toxic substances. The potential utility of {99m}Tc-1-thio-D-glucose for tumor imaging was studied in vitro and in vivo models. The present study demonstrated that {99m}Tc-1-Thio-D-glucose is a prospective radiopharmaceutical for cancer visualization

Study of potential utility of new radiopharmaceuticals based on technetium-99m labeled derivative of glucose

Purpose: to study the potential utility of 1-thio-D-glucose labeled with {99m}Tc for cancer imaging in laboratory animals. Materials and method: the study was carried out in cell cultures of normal CHO (Chinese hamster ovary cells CHO) and malignant tissues MCF-7 (human breast adenocarcinoma MCF-7). To evaluate the uptake of {99m}Tc-1-thio-D-glucose in normal and tumor tissue cells, 25 MBq of 1-thio-D-glucose labeled with {99m}Tc was added to the vials with 3 million cells and incubated for 30 min at room temperature. After centrifugation of the vials with cells, the supernatant was removed. The radioactivity in vials with normal and tumor cells was then measured. In addition, the study included 40 mice of C57B1/6j lines with tumor lesion of the right femur. For neoplastic lesions, Lewis lung carcinoma model was used. Following anesthesia, mice were injected intravenously with 25 MBq of {99m}Tc-1-thio-D-glucose. Planar scintigraphy was performed 15 minutes later in a matrix of 512x512 pixels for 5 min. Results: when measuring the radioactivity of normal and malignant cells after incubation with {99m}Tc-1-thio-D-glucose, it was found that the radioactivity of malignant cells was higher than that of normal cells. The mean values of radioactivity levels in normal and malignant cells were 0.3±0.15 MBq and 1.07±0.6 MBq, respectively. All examined animals had increased accumulation of {99m}Tc-1-thio-D-glucose at the tumor site. The accumulation of {99m}Tc-1-thio-D-glucose in the tumor was on average twice as high as compared to the symmetric region. Conclusion: The present study demonstrated that {99m}Tc-1-thio-D-glucose is a prospective radiopharmaceutical for cancer visualization. In addition, high accumulation of {99m}Tc-1-thio-D-glucose in the culture of cancer cells and in tumor tissue of animals demonstrates tumor tropism of the radiopharmaceutical

The Foundations of the Development of Technologies of the Synthesis of Radiopharmaceuticals

The selection of precursors (for example chelating agents) and development of a technique of chemical modification of the target molecules retaining its ability to bind to specific receptors are very important in the synthesis of radiopharmaceuticals. As some important precursors for target radiopharmaceuticals omega-iodo-aliphatic carboxylic acids and their esters can be used. We have developed an environmentally safe process for producing omega-iodoaliphatic carboxylic acids and their esters of the available, inexpensive and low toxic aliphatic cyclic ketones. We proposed a new method for the synthesis of the chelating agents omega-thia- or (bis(2-hydroxyethyl)amino)- aliphatic carboxylic acids (chelate 1 and chelate 2), which was caused by the existing disadvantages in the existing methods. Thus, based on our method the precursors (chelates) with yield of over 70-90% on the final stage were synthesized, and then the high effectiveness in producing target radiopharmaceuticals using different biomolecules was showed. 99mTc-chelates complexes were prepared with radiochemical purity >91% and found to be stable at room temperature for six hours

In Vitro Evaluation of a Specific Radiochemical Compound Based on 99mTc-labeled DARPinG3 for Radionuclide Imaging of Tumors Overexpressing Her-2/neu

It is still necessary to search for new informative diagnostic methods to detect malignant tumors with overexpression of Her-2/neu, which are characterized by the aggressive course of the disease, rapid rate of tumor growth and low rates of relapse-free and overall survival. In recent years, the radioisotope techniques for detection of specific tumor targets have been developing actively. Purpose: to develop a chemically stable radiochemical compound for the targeted imaging of cells overexpressing Her-2/neu. Material and methods: The study was performed using 2 cell lines .The human breast adenocarcinoma HER2-overexpressing cell line BT-474 was chosen to detect specific binding. As a control, HER2-negative human breast adenocarcinoma MCF-7 was used. The human breast adenocarcinoma BT-474 and MCF-7 cell lines were seeded in chamber-slides at the density of 35,000 cells/ml in trypsin-EDTA (PanEco) medium and grown overnight at 37°C. After that both cell lines were washed with Phosphate buffered saline (PBS) and distributed into test tubes to 1 ml (5 millions cells in each). After adding 100 [mu]l (70 MBq) studied complex of 99mTc-DPAH-DARPinG3 was incubated for 40 min at +4°C. Washing was performed three times with buffer PBS and 5% Bovine Serum Albumin (BSA). The characteristics of the binding specificity of the test set with the HER-2/neu receptor were determined by direct radiometric and planar scintigraphy. Nonparametric Mann-Whitney test was used to assess the differences in the quantitative characteristics between groups. Results: The output of the labeled complex was more than 91%, with a radiochemical purity of more than 94%. When carrying out a visual scintigraphic assessment much greater intensity accumulation of radiotracer was observed in the studied cell culture surface receptor overexpressing Her-2/neu. The results of direct radiometric also showed higher accumulation of the radiopharmaceutical in the adenocarcinoma cell line BT-474 human breast cancer overexpressing Her-2/neu compared to the control group. Conclusion: The preclinical studies demonstrated a high in vitro stability of the study compound, as well as its accumulation in the cell group overexpressing Her-2/neu

Development and Study of {99m}Tc-1-Thio-D-glucose for Visualization of Malignant Tumors

The preclinical studies of {99m}Tc-1-Thio-D-glucose, a new tumor-seeking agent based on technetium-99mlabeled glucose derivative, were conducted, and the feasibility of using this radiopharmaceutical for tumor visualization was studied. The preclinical studies were carried out strictly in accordance with the local legislation and were regulated by the generally accepted research standards. {99m}Tc-1-Thio-D-glucose was found to have optimal pharmacokinetic and physico-chemical properties for diagnostic imaging and was proved to belong to the low-toxic substances. The potential utility of {99m}Tc-1-thio-D-glucose for tumor imaging was studied in vitro and in vivo models. The present study demonstrated that {99m}Tc-1-Thio-D-glucose is a prospective radiopharmaceutical for cancer visualization

The study of interaction of modified fatty acid with {99m}Tc in alcoholic media

The paper presents the results of laboratory research aimed at the development of methods of synthesis of new radiodiagnostic agents based on modified fatty acid labelled with technetium-99m intended for scintigraphic evaluation of myocardial metabolism. In particular, the interaction of substance with {99m}Tc in alcoholic media and the use of ethanol as solvent in the synthesis of the radiopharmaceutical were studied

Experimental study of radiopharmaceuticals based on technetium-99m labeled derivative of glucose for tumor diagnosis

Purpose: to study the potential utility of 1-thio-D-glucose labeled with 99mTc for cancer imaging in laboratory animals. Materials and method: the study was carried out in cell cultures of normal CHO (Chinese hamster ovary cells CHO) and malignant tissues MCF-7 (human breast adenocarcinoma MCF-7). To evaluate the uptake of 99mTc-1-thio-D-glucose in normal and tumor tissue cells, 25 MBq of 1-thio-D-glucose labeled with 99mTc was added to the vials with 3 million cells and incubated for 30 minutes at room temperature. After centrifugation of the vials with cells, the supernatant was removed. Radioactivity in vials with normal and tumor cells was then measured. In addition, the study included 40 mice of C57B 1/6j lines with tumor lesion of the right femur. For neoplastic lesions, Lewis lung carcinoma model was used. Following anesthesia, mice were injected intravenously with 25MBq of 99mTc-1-thio-D-glucose. Planar scintigraphy was performed 15 minutes later in a matrix of 512x512 pixels for 5 minutes. Results: when measuring the radioactivity of normal and malignant cells after incubation with 99mTc-1-thio-D- glucose, it was found that the radioactivity of malignant cells was higher than that of normal cells. The mean values of radioactivity levels in normal and malignant cells were 0.3±0.15MBq and 1.07±0.6MBq, respectively. All examined animals had increased accumulation of 99mTc-1-thio- D-glucose at the tumor site. The accumulation of 99mTc-1-thio-D-glucose in the tumor was on average twice as high as compared to the symmetric region. Conclusion: The present study demonstrated that 99mTc-1-thio-D-glucose is a prospective radiopharmaceutical for cancer visualization. In addition, high accumulation of 99mTc-1-thio-D-glucose in the culture of cancer cells and in tumor tissue of animals demonstrates tumor tropism of the radiopharmaceutical