The paper presents the procedure for planning an experiment to create standard sets of reagents for a technetium-99m generator based on glucose derivatives. All stages are presented from researching the required quantities of a substance, a reducing agent, a stabilizer and auxiliary components to developing lyophilized kits and conducting quality control. The radiochemical purity of radiopharmaceuticals prepared on the basis of the developed kits ranged from 90.0 to 99.0%. We also showed the functional suitability of the developed preparations on C57B1/6j mice with an implanted malignant tumor -Lewis lung carcinoma. open Scientific RepoRtS | (2020) 10:5121 | https://doi.org/10.1038/s41598-020-61707-7 www.nature.com/scientificreports www.nature.com/scientificreports/ 0.2 Pa and a condenser temperature of −50 °C for at least 24 h, including 4 h of drying in the upper chamber. For the radiolabeling 4 mL of sodium pertechnetate solution [ 99m Tc] with an activity of 1.0 GBq was added to the obtained lyophilized samples and incubated at room temperature for 30 min. Radiochemical purity (RCP) control and the formation of the complex were monitored by TLC. D-glucosamine labeling. Preparation of lyophilizates of D-glucosamine substances was carried out as follows: 1 mL of a solution containing 20 mg of the glucose derivative, 0.140 mg of tin chloride and 200 μl of hydrochloric acid with a concentration of 0.05 mole was placed in a 10 mL vial. The vials without prior freezing were applied to a freeze-dryer at a pressure of 0.2 Pa and a condenser temperature of −50 °C for at least 24 h, including 4 h of drying in the upper chamber. For the radiolabeling 4 mL of sodium pertechnetate solution [ 99m Tc] with an activity of 1.0 GBq was added to the obtained lyophilized samples and incubated at room temperature for 30 min. Radiochemical purity (RCP) control and the formation of the complex were monitored by TLC. Scientific RepoRtS | (2020) 10:5121 | https://doi.www.nature.com/scientificreports www.nature.com/scientificreports/ particular, high-performance liquid chromatography (HPLC) are most frequently used for their determination 16 and for semiquantitative determination -thin-layer chromatography 17 .In our experiments, a high-pressure liquid chromatograph "Agilent 1200" with a refractometric and UV detectors and two types of columns ZORBAX NH2 and ZORBAX SB-C18 using different elution modes.As shown by our research method 1 using a UV detector, ZORBAX SB-C18 columns and gradient elution mode cannot be applied to preparations based on 5-thio-D-glucose and 1-thio-D-glucose, i.e. ascorbic acid, which in this mode of determination is not separated from the main substance and significantly increases the Name of the parameter RP "5-thio-Dglucose, 99m Тс" RP "1-thio-Dglucose, 99m Тс" RP «"Dglucosamine, 99m Тс" Volume of mixture in 1 flask Not more than 1 ml Not more than 1 ml Not more than 1 ml Scientific RepoRtS | (2020) 10:5121 | https://doi.
Abstract. 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-Dglucose 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 512 512 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 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 work considers the problem of obtaining nanocolloid radiopharmaceuticals (RPs) and studying their functional suitability for diagnosing sentinel lymph nodes (SLN) in cancer patients. Two principal approaches to the formation of technetium-99m-labeled particles based on inorganic and organic matrices were considered when carrying out research to develop methods for the production of nanocolloid RPs. The composition of the reagents and the conditions for obtaining nanocolloid radiopharmaceuticals were determined. The functional suitability of new RPs for scintigraphic diagnostics of sentinel lymph nodes has been studied. The identification of sentinel lymph nodes-the first nodes that stand in the way of metastasizing of malignant neoplasms attracts increasing interest in modern oncological practice 1-5. It is believed that if the SLN is not affected by the metastatic process, then all other regional lymph nodes are intact, so the results of biopsy of these nodes are an objective diagnostic criterion for the spread of malignant process (Fig. 1). The optimal method of detecting SLN is the use of colloid nanomaterials labeled with technetium-99m for scintigraphic or radiometric determination of node localization 6-13. Not so much the chemical nature of such particles but their size is the determining factor in the choice of the indicator in this case. Thus, according to Schauer 14 , a colloid with a particle size of less than 50 nm can accumulate not only in the SLN, but also at nodes of 2 and 3 orders of magnitude. Particles with the sizes of more than 100 nm slowly migrate from the injection site. The colloid with the particle size from 50 to 80 nm was recognized as the optimal one for detecting SLN. The simplest method of obtaining colloids with given sizes and properties is immobilization of 99m Tc on the surface of nanosized materials. Technetium-99m is by far the most popular radionuclide for conducting diagnostic studies, practically in all fields of medicine 15-18. This is primarily due to its nuclear-physical characteristics: a relatively short half-life (6.02 h) and γ-radiation energy of 0.1405 meV, providing a low exposure dose and, at the same time, sufficient penetrating power for radiometric measurements. Today, the Tc-99m Tilmanocept radiopharmaceutical is widely used, which has proven itself well and gives good results. But its production is quite time-consuming and requires expensive components. We offer a less laborious method from the simple components 19,20. Materials and methods Materials. All the reagents were purchased from Sigma-Aldrich ACS grade and used without further purification. Technetium-99m was obtained from chromatographic 99 Mo/ 99m Tc generator " 99m Tc-GT-TOM" produced by Tomsk Polytechnic University (TPU)-Tomsk, Russia. Three types of nanoparticles were selected to obtain nanocolloids labeled with 99m Tc. The first type of colloids was created on the basis of metal chelates with chemically modified complexons of diethylenetriaminepentaacetic acid (DTPA). It should be noted tha...
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