Synthesis, Quality Control and Bio-evaluation of 99mTc-cyclophosphamide

Abstract

Cancer is found to be the leading cause of death worldwide characterized by uncontrolled cell division. Nuclear medicines imaging by 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, labelling of CPH with Tc-99m is performed for diagnostic purpose, which gave labelling yield as high as 99% by using 20μg SnCl₂.2H₂O, 200μg of ligand at pH 7 for 10 min reaction time at room temperature. The characterization of the prepared complex was performed by using ITLC, electrophoresis and HPLC. In vitro stability was analyzed in the presence of human serum at 37^◦C which have maximum value of 94±0.5. The biodistribution studies of ^99mTc-CPH were performed in normal and tumor bearing Swiss Webster mice. The high accumulation of ^99mTc-CPH was observed in liver and tumours respectively at 4h after injection. Biodistribution results revealed that ^99mTc-CPH may be a potential tumour diagnostic agent simultaneously with chemotherapy.

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The ^99mTc-labled-CPH was prepared very efficiently through a simple method. Biodistribution results revealed that ^99mTc-CPH may be a potential tumour diagnostic agent simultaneously with chemotherapy.

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