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Background and Objective: Hypoxia is an important biological characteristics of solid tumor, it is not sensitive to radiotherapy and chemotherapy for which is the presence of hypoxic cell, thus increasing their resistance to conventional radiotherapy and chemotherapy, therefore, the detection of hypoxia degree of tumor tissue is of great significance. The hypoxia imaging of nuclear medicine can reflect the degree of tissue hypoxia, which can selectively retained on the hypoxic cells or tissues, including nitroimidazole and non nitroimidazole; the nitroimidazole is widely and deeply researched as hypoxic celles developer in China and abroad at present. The research about application of radionuclide labelled technique has clinical application value to develop the hypoxia imaging agent EDTA-MN complexes which was labeled. To study the feasibility of (99m)Tc by direct labeling method, the radiochemical properties evaluation of (99m)Tc-EDTA-MN, and observe the distribution characteristics of (99m)Tc radiolabeled EDTA-MN in the xenograft lung cancer nude mice bearing non-small cell lung cancer cell (A549), and provide experimental evidence for its further research and application., Methods: The radiolabeling of EDTA-MN with (99m)Tc was performed with direct labeling method, respectively, on the reaction dosage (10 mg, 5 mg, 2 mg), stannous chloride dosage (8 mg/mL, 4 mg/mL, 2 mg/mL), mark system pH (2, 4, 5, 6) one by one test, using orthogonal design analysis, to find the optimal labeling conditions. Labelling rate, radiochemical purity, lipid-water partition coefficient and in vitro stability in normal saline (NS) were determined by TLC and HPLC, and the preliminary study on the distribution of (99m)Tc-EDTA-MN in nude mice., Results: The labeling rate of 99mTc-EDTA-MN with the best labeling conditions was (84.11±2.83)%, and the radiochemical purity was higher than 90% by HPLC purification, without any notable decomposition at room temperature over a period of 12 h. The partition coefficient was lgP=-3.05, indicated that this complex was hydrophilic. At 3 h post-injection, the imaging of (99m)Tc-EDTA-MN in nude mice bearing non-small cell lung cancer cell showed that more radioactive gathered in bladder at 0.5 h, the transplanted tumor was clearly imaged at 1 h post-injection, during whole imaging radioactive in other tissues and organs was low. The radioactivity of tumor uptake by using of ROI technology were (88.14±11.59), (123.17±9.06), (98.08±14.40) and (79.87±10.57) at 0.5, 1, 2, 3 h post-injection, and the ratio of T/NT of tumor and liver area were (1.95±0.19), (3.58±0.78), (3.95±0.39) and (5.01±0.28), respectively. (99m)Tc-EDTA-MN could be quickly cleared from the blood in mice primarily through the kidneys, and the radioactivity in other tissues and organs remained low., Conclusions: (99m)Tc-EDTA-MN can be easily prepared and labeled compound with high labeling rate and stability, it appears to be suitable for further experiments requirement in vivo and in vitro application.

Background: Lung cancer is a malignant tumor with high mortality rates. This study aims to develop potential candidates of integrin αvβ3 imaging agents, which can facilitate the diagnosis and treatment of lung cancer., Methods: The T7 peptide was labeled with carbonyl technetium. The thin layer chromatography with acetone as the development system was performed to investigate the purity and stability of (99m)Tc-T7. The binding affinity of (99m)Tc-T7 with NCI-H157 tumor cells was determined. The biodistribution of (99m)Tc-T7 in nude mice bearing non-small cell lung carcinoma was observed after injection of (99m)Tc-T7 at 0.5 h, 1 h, 2 h, 4 h, and 8 h, and the radioactive ratio of tumor (T) and non-tumor tissues (NT) was calculated., Results: 99mTc labeled T7 had high radiochemical purity of more than 90%, which does not require further purification, with good stability in vitro. The association and dissociation constant (KD) of (99m)Tc-T7 with NCI-H157 tumor cells was 196.1 nM. (99m)Tc-T7 was mainly metabolism through the internal organs with rapid blood removal. Moreover, the uptake in tumor tissue was significantly higher than the muscle with tumor/muscle ratio of 5.8. In addition, the (99m)Tc-T7 exhibited a transient accumulation in the lungs., Conclusions: The (99m)Tc-T7 could be prepared using a simple method, had high labeling rate and good stability, and could be accumulated at tumor site. Thus, (99m)Tc-T7 is a potential lung cancer SPECT/CT imaging agent.

Objective: To investigate the biological character of new agent 153Sm-citrate-nano-Hydroxyapatite (nano-HA) in vitro and in vivo, and to explore a new radiopharmaceutical for the target therapy of bone metastasis cancer., Methods: The nano-HA was synthesized by collosol-gelatum method, and evaluated by transmission electron microscopy (TEM) and X-ray diffraction (XRD). 153Sm was produced at a high specific activity and excellent radionuclidic purity, with which nano-HA was labeled by citrate transfer ligands in the best environment. By adopting the independent variable method, we also studied the optimally labeled condition and stability of 153Sm-citrate-nano-HA in vitro. And 153Sm-citrate-nano-HA was injected into normal rabbits for radio scanning performed. The cancer cell SMMC-7721 and MCF-7 cell lines were divided into two groups, and treated with nano-HA, 153Sm-citrate and 153Sm-citrate-nano-HA in vitro respectively, of which the cell survival rate was measured by MTT methods., Results: Through the detections of TEM, XRD showed that nano-HA consisted of needle-like microcrystals. The label rate of 153Sm-citrate-nano-HA was more than 95%, and extremely stable in vitro. The radio scanning of normal rabbits showed the skeletal system to be clear, and other systems, for example liver, spleen and kidney, could also be seen. The cell culture experiments in vitro indicated that 153Sm-citrate-nano-HA strongly inhibited the proliferation of SMMC-7721 and MCF-7 cells. 153Sm-citrate-nano-HA's half effective inhibition concentrations were 1.89 mg/L and 0.094 mg/L respectively; nano-HA's half effective inhibition concentrations were 3. 31 mg/L and 0.52 mg/L respectively; 153Sm-citrate's half effective inhibition concentrations were 4. 32 mg/L and 0. 67 mg/L respectively., Conclusions: Sm-citrate-nano-HA shows fine biological properties, and is well worth for further researched and prepared as a promising potential radiopharmaceutical in nuclidic treatment for cancer bone metastases.

Objective: To explore the methods for labeling CDTPA-coupled CD45 monoclonal antibody (mAb) with yttrium-90 ((90)Y) for potential acute myeloid therapy., Methods: CD45 mAb was labeled with (90)Y by CDTPA and the labeling rate, radiochemical purity, final specific activity, and immunological activity of the mAb were detected., Results: With the optimal molar ratio of CDTPA/Ab at 20:1, the labeling rate was 95%, radiochemical purity 99.8%, and final specific activity 1.9 mCi/mg. This conjugate was stable in vitro with comparable immunological activity in comparison with unlabeled CD45 mAb., Conclusion: (90)Y-CDTPA-CD45 mAb possesses good properties as an ideal targetting therapeutic agent for acute leukemia.