Motaleb M.A.El-Safoury D.M.Abd-Alla W.H.Awad G.A.S.Sakr T.M.Labelled Compounds DepartmentHot Labs CenterAtomic Energy AuthorityCairoEgypt; Pharmaceutical Chemistry DepartmentCollege of Pharmaceutical Sciences and Drug ManufacturingMisr University for Science & TechnologyGizaEgypt; Pharmaceutics and Industrial Pharmacy DepartmentFaculty of PharmacyAin Shams UniversityCairoEgypt; Radioactive Isotopes and Generator DepartmentHot Labs CenterAtomic Energy AuthorityCairoEgypt; Pharmaceutical Chemistry DepartmentFaculty of PharmacyOctober University of Modern Sciences and Arts (MSA)GizaEgypt2020-01-092020-01-0920189553002https://doi.org/10.1080/09553002.2019.1524945PubMed ID 30373490https://t.ly/nv3MnScopusMSA Google ScholarPurpose: Ifosfamide as a chemotherapeutic drug is used for the treatment of different cancer types. The purpose of this study is the preparation of 99mTc-ifosfamide complex to be evaluated as a potential candidate for tumor imaging. Materials and methods: The radiolabeling of ifosfamide with technetium-99m was carried out by mixing 4mg ifosfamide and 5 ?g of SnCl2.2H2O with 400 MBq Na99mTcO4 at pH 9 for 30 min at room temperature. Computer simulation studies were performed using Accelrys Discovery Studio 2.5 operating system to illustrate the interaction of ifosfamide and 99mTc-ifosfamide complexes with DNA. The in-vivo biodistribution of 99mTc-ifosfamide was studied in tumor-bearing Albino mice. Results: A new 99mTc-ifosfamide complex was synthesized with a good radiochemical yield of 90.3. 2.1% under the optimized conditions and exhibited in-vitro stability up to 2 h. Biodistribution studies showed good uptake in tumor site and high uptake in tumor site with T/NT ?3 after 60 min post-injection. Besides, the molecular docking study confirmed that the complexation of ifosfamide with technetium-99m does not abolish its binding to the target receptor. Conclusion: These promising results afford a new radiopharmaceutical that could be used as a potential tumor imaging. 2018, Copyright 2018 Taylor & Francis Group, LLC.EnglishOctober University for Modern Sciences and Artsجامعة أكتوبر للعلوم الحديثة والآدابUniversity of Modern Sciences and ArtsMSA UniversityIfosfamideimaginglabelingtechnetium-99mtumor targetingifosfamideifosfamide complex tc 99mradiopharmaceutical agenttechnetium 99munclassified drugDNA topoisomeraseifosfamidetechnetiumanimal experimentanimal modelanimal tissueArticlecomplex formationcomputer simulationcontrolled studydrug distributiondrug DNA interactiondrug screeningdrug stabilitydrug synthesisfemalein vitro studyin vivo studyisotope labelingmolecular dockingmolecular imagingmolecular modelmousenonhumanpriority journalradiochemistrysolid malignant neoplasmanimalchemistryhumankineticsmetabolismmolecular dockingmolecular imagingproceduresprotein domainsynthesistissue distributionAnimalsDNA Topoisomerases, Type IDrug StabilityHumansIfosfamideKineticsMiceMolecular Docking SimulationMolecular ImagingProtein DomainsRadiochemistryTechnetiumTissue DistributionArticlehttps://doi.org/10.1080/09553002.2019.1524945PubMed ID 30373490