Cancer biotherapy & radiopharmaceuticals · 2007
Preparation and imaging research on 188Re-DTPA-deoxyglucose in MCF-7 tumor-bearing mice.
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Chen Yue, Xiong Qingfeng, Yang Xiqun, Huang Zhanwen, He Ling
Аннотация
OBJECTIVE: To investigate the preparation of (188)Re-diethylenetriaminepentaacetic acid-2-deoxyglucose ((188)Re-DTPA-DG) and its imaging quality and therapeutic effect.
METHODS: Labeling of DTPA-DG with (188)Re was performed in the presence of stannous ion and sodium D-gluconate at a pH of 5.5 with 3 hours of incubation at 37 degrees C. The radiolabeling yields of (188)Re-DTPA-DG were determined by paper chromatography with a solution of acetone and saline (0.9% NaCl) as a developing agent. The imaging quality of (188)Re-DTPA-DG was determined by injecting 0.1 mL of a preparation having a radioactivity of 92.5GBq/L into the tail vein of nude mice bearing MCF-7 mammary tumors and imaging the tumors at 2, 4, 8, 12, and 24 hours after injection of the radiolabeled agent. Tumor volume was recorded every 2 or 3 days for 21 days.
RESULTS: The radiochemical purity of the (188)Re-DTPA-DG complex was 95.0%. In the imaging study, the tumor-to-nontumor-tissue ratios (T/NT) of radioactivity at 12 and 24 hours after intravenous injection of the radiolabeled agent were 5.9 and 7.8, respectively. The tumor volume in the (188)Re-DTPA-DG-treated group of mice increased more slowly than that in the control group, and the two groups differed greatly in this measure at 21 days, with tumor volumes of 823.6 +/- 50.58 mm(3) and 1162.7 +/- 73.08 mm(3) in the (188)Re-DTPA-DG treated and control groups, respectively (p < 0.01).
CONCLUSIONS: (188)Re-DTPA-DG showed excellent tumor targeting and tumor-growth-suppressing effects, and holds promise as an internal agent for tumor radiotherapy.
METHODS: Labeling of DTPA-DG with (188)Re was performed in the presence of stannous ion and sodium D-gluconate at a pH of 5.5 with 3 hours of incubation at 37 degrees C. The radiolabeling yields of (188)Re-DTPA-DG were determined by paper chromatography with a solution of acetone and saline (0.9% NaCl) as a developing agent. The imaging quality of (188)Re-DTPA-DG was determined by injecting 0.1 mL of a preparation having a radioactivity of 92.5GBq/L into the tail vein of nude mice bearing MCF-7 mammary tumors and imaging the tumors at 2, 4, 8, 12, and 24 hours after injection of the radiolabeled agent. Tumor volume was recorded every 2 or 3 days for 21 days.
RESULTS: The radiochemical purity of the (188)Re-DTPA-DG complex was 95.0%. In the imaging study, the tumor-to-nontumor-tissue ratios (T/NT) of radioactivity at 12 and 24 hours after intravenous injection of the radiolabeled agent were 5.9 and 7.8, respectively. The tumor volume in the (188)Re-DTPA-DG-treated group of mice increased more slowly than that in the control group, and the two groups differed greatly in this measure at 21 days, with tumor volumes of 823.6 +/- 50.58 mm(3) and 1162.7 +/- 73.08 mm(3) in the (188)Re-DTPA-DG treated and control groups, respectively (p < 0.01).
CONCLUSIONS: (188)Re-DTPA-DG showed excellent tumor targeting and tumor-growth-suppressing effects, and holds promise as an internal agent for tumor radiotherapy.