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S.b. Challan, Ph.d., S.i. Khater, A.m. Rashad,
Volume 20, Issue 3 (7-2022)
Abstract

Background: Radiolabeling process has a very important role in prediction of in-vivo biodistribution. Moreover, biodistribution is considered the backbone of the recent discovery of anti-cancer drugs.Technetium-99m has been the most utilized radionuclide in nuclear medicine due to its optimal physical characteristics. Materials and Methods: Oseltamivir(Osel) was radiolabeled by technetium-99m under reductive conditions directly.1.5 mg of Osel was followed by 25 μg of SnCl2. H2O, 200 μl buffer pH 4 at 60ºC reaction temperature, and the reaction time was 30 minutes. In-vivo biodistribution of 99mTc-Oseltamivir (99mTc-Osel) tracer was studied using tumor-bearing Albino mice compared to control. The radiochemical purity percentage was calculated using the ascending paper chromatography technique and also, confirmed by paper electrophoresis before the in-vivo biodistribution in mice.99mTc-Osel tracer was further analyzed utilizing high performance liquid chromatography analysis .Spartan software for molecular modeling is used for optimizing the different complex patterns of Osel with 99mTc where energy was minimized using the semi-empirical method with a PM3 basis set. Result: 99mTc-Osel tracer was synthesized with a good yield of 98.7±0.34% at the optimized conditions and the preparation exhibited in-vitro stability up to 3 h. In vivo biodistribution studies showed high uptake in tumor cells with the target to the non-target ratio of 4.55±0.2 after 3 h. post- injection. Conclusion: 99mTc-Osel tracer focuses on the tumor site with a high percentage appropriate to use 99mTc-Osel as a useful tool for tumor imaging.


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International Journal of Radiation Research
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