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

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 use of (99m}Tc-Al[2]O[3] for detection of sentinel lymph nodes in breast cancer

Purpose: to study the feasibility of using the new radiopharmaceutical based on the technetium-99m-labeled gamma-alumina for identification of sentinel lymph nodes (SLNs) in breast cancer patients. The study included two groups of breast cancer patients who underwent single photon emission computed tomography (SPECT) and intraoperaive gamma probe identification of sentinel lymph nodes (SLNs). To identify SLNs, the day before surgery Group I patients (n=34) were injected with radioactive {99m}Tc-Al[2]O[3], and Group II patients (n=30) received 99mTc-labeled phytate colloid. A total of 37 SLNs were detected in Group I patients. The number of identified SLNs per patient ranged from 1 to 2 (the average number of identified SLNs was 1.08). Axillary lymph nodes were the most common site of SLN localization. 18 hours after {99m}Tc-Al[2]O[3] injection, the percentage of its accumulation in the SLN was 7-11% (of the counts in the injection site) by SPECT and 17-31% by gamma probe detection. In Group II SLNs were detected in 27 patients. 18 hours after injection of the phytate colloid the percentage of its accumulation in the SLN was 1.5-2% out of the counts in the injection site by SPECT and 4-7% by gamma probe. The new radiopharmaceutical based on the {99m}Tc-Al[2]O[3] demonstrates high accumulation in SLNs without redistribution through the entire lymphatic basin. The sensitivity and specificity of {99m}Tc-Al[2]O[3] were 100% for both SPECT and intraoperative gamma probe identification

The use of (99m}Tc-Al[2]O[3] for detection of sentinel lymph nodes in breast cancer

Purpose: to study the feasibility of using the new radiopharmaceutical based on the technetium-99m-labeled gamma-alumina for identification of sentinel lymph nodes (SLNs) in breast cancer patients. The study included two groups of breast cancer patients who underwent single photon emission computed tomography (SPECT) and intraoperaive gamma probe identification of sentinel lymph nodes (SLNs). To identify SLNs, the day before surgery Group I patients (n=34) were injected with radioactive {99m}Tc-Al[2]O[3], and Group II patients (n=30) received 99mTc-labeled phytate colloid. A total of 37 SLNs were detected in Group I patients. The number of identified SLNs per patient ranged from 1 to 2 (the average number of identified SLNs was 1.08). Axillary lymph nodes were the most common site of SLN localization. 18 hours after {99m}Tc-Al[2]O[3] injection, the percentage of its accumulation in the SLN was 7-11% (of the counts in the injection site) by SPECT and 17-31% by gamma probe detection. In Group II SLNs were detected in 27 patients. 18 hours after injection of the phytate colloid the percentage of its accumulation in the SLN was 1.5-2% out of the counts in the injection site by SPECT and 4-7% by gamma probe. The new radiopharmaceutical based on the {99m}Tc-Al[2]O[3] demonstrates high accumulation in SLNs without redistribution through the entire lymphatic basin. The sensitivity and specificity of {99m}Tc-Al[2]O[3] were 100% for both SPECT and intraoperative gamma probe identification

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

99mTc-labeled monosaccharide kits: development methods and quality control

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

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%

Experimental study of {99m}Tc-aluminum oxide use for sentinel lymph nodes detection

The purpose of the study was a comparative research in the possibility of using the radiopharmaceuticals {99m}Tc-Al[2]O[3] and {99m}Tc-Nanocis for visualizing sentinel lymph nodes. The measurement of the sizes of {99m}Tc-Al[2]O[3] and {99m}Tc-Nanocis colloidal particles was performed in seven series of radiopharmaceuticals. The pharmacokinetics of {99m}Tc-Al[2]O[3] and {99m}Tc-Nanocis was researched on 50 white male rats. The possibility of the use of {99m}Tc-Al[2]O[3] and {99m}Tc-Nanocis for lymphoscintigraphy was studied in the experiments on 12 white male rats. The average dynamic diameter of the sol particle was 52-77 nm for {99m}Tc-Al[2]O[3] and 16.7-24.5 nm for {99m}Tc-Nanocis. Radiopharmaceuticals accumulated in the inguinal lymph node in 1 hour after administration; the average uptake of {99}mTc-Al[2]O[3] was 8.6% in it, and the accumulation of {99m}Tc-Nanocis was significantly lower-1.8% (p < 0.05). In all study points the average uptake of {99m}Tc-Al[2]O[3] in the lymph node was significantly higher than {99m}Tc-Nanocis accumulation. The results of dynamic scintigraphic studies in rats showed that {99m}Tc-Al[2]O[3] and {99m}Tc-Nanocis actively accumulated into the lymphatic system. By using {99m}Tc-Al[2]O[3] inguinal lymph node was determined in 5 minutes after injection and clearly visualized in all the animals in the 15th minute, when the accumulation became more than 1% of the administered dose. Further observation indicated that the {99m}Tc-Al[2]O[3] accumulation reached a plateau in a lymph node (average 10.5%) during 2-hour study and then its accumulation remained practically at the same level, slightly increasing to 12% in 24 hours. In case of {99m}Tc-Nanocis inguinal lymph node was visualized in all animals for 15 min when it was accumulated on the average 1.03% of the administered dose. Plateau of {99m}Tc-Nanocis accumulation in the lymph node (average 2.05%) occurred after 2 hours of the study and remained almost on the same level (in average 2.3%) for 24 hours. Thus, the experimental study of a new domestic radiopharmaceutical showed that the {99m}Tc-Al[2]O[3]accumulates actively in the lymph nodes several times as compared to the imported analogue and its practical application will facilitate intraoperative identification of sentinel lymph nodes