Radiosynthesis, molecular modeling studies and biological evaluation of 99m Tc-Ifosfamide complex as a novel probe for solid tumor imaging.

PURPOSE: Ifosfamide as a chemotherapeutic drug is used for the treatment of different cancer types. The purpose of this study is the preparation of 99m Tc-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 μg of SnCl2 .2H2 O with 400 MBq Na99m TcO4 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 99m Tc-ifosfamide complexes with DNA. The in-vivo biodistribution of 99m Tc-ifosfamide was studied in tumor-bearing Albino mice.

RESULTS: A new 99m Tc-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.