Synthesis, quality control, and bio-evaluation of 99m Tc-cyclophosphamide.

Cancer is found to be the leading cause of death worldwide characterized by uncontrolled cell division. Nuclear medicines imaging using radiopharmaceuticals have pronounced potential for the diagnosis and treatment of cancers. Cyclophosphamide (CPH) is an antineoplastic drug which targets selectively cancer cells. In the present work, labeling of CPH with Tc-99m is performed for diagnostic purpose, which gave labeling yield as high as 99% using 20 μg SnCl ₂ ·2H ₂ O, 200 μg of ligand at pH 7 for 10 min reaction time at room temperature. The characterization of the prepared complex was performed using ITLC, electrophoresis, and HPLC. In vitro stability was analyzed in the presence of human serum at 37°C which has maximum value of 94 ± 0.5. The biodistribution studies of ^99m Tc-CPH were performed in normal and tumor bearing Swiss Webster mice. The high accumulation of ^99m Tc-CPH was observed in liver and tumours respectively at 4 hr after injection. Biodistribution results revealed that ^99m Tc-CPH may be a potential tumour diagnostic agent simultaneously with chemotherapy.
(© 2017 John Wiley & Sons A/S.)