Abstract
In this study, the radiocomplexation of risedronic acid, a potent bisphosphonate with a no carrier added (NCA) 177 Lu, was investigated and followed by quality control studies, biodistribution evaluation, and dosimetry study for human based on biodistribution data in Wistar rats. The moderate energy β- emitter, 177 Lu (T½ =6.7days, Eβmax =497keV), has been considered as a potential agent for development of bone-seeking radiopharmaceuticals. Because the specific activity of the radiolabeled carrier molecules should be high, the NCA radionuclides have an effective role in nuclear medicine. Many researchers illustrated an NCA 177 Lu production; among these separation techniques, extraction chromatography has been considered more capable than other methods. The NCA 177 Lu was produced with specific activity of 48Ci/mg and radionuclidic purity of 99.99% by the irradiation of enriched 176 Yb target in thermal neutron flux of 4×1013 n·cm-2 ·s-1 for 14days. The NCA 177 Lu was mixed to a desired amount of sodium risedronate (15mg/mL, 200μL) and incubated with stirring at 95°C for 30minutes. The radiochemical purity of 177 Lu-risedronate was determined by radio thin-layer chromatography, and high radiochemical purities (>97%) were obtained under optimized reaction conditions. The complex was injected to Wistar rats, and complex biodistribution was performed 4hours to 7days postinjections showing high bone uptake (9.8%±0.24% ID/g at 48hours postinjection). Also, modeling the radiation dose delivery by RADAR software for the absorbed dose evaluation of each human organ showed a major accumulation of the radiocomplex in bone tissue.
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