Synthesis of a Potential Tumor Imaging Agent by Oxidative Radioiodination of Aspirin and Its Preclinical Study

Abstract

Aspirin, one of nonsteroidal anti-inflammatory analgesic drugs, was labeled with ¹²⁵I with a labeling yield of 85.5% under the following conditions: pH 9, 100 mg of the substrate, 50 µg of Chloramine-T, 5–15 min, room temperature. The radiochemical yield of ¹²⁵I-aspirin was determined by paper chromatography and electrophoresis, and the radiochemical purity was determined by HPLC.¹²⁵I-aspirin was stable for at least 3 h. Biodistribution of ¹²⁵I-aspirin in normal and tumor-bearing mice was studied. The uptake of ¹²⁵I-aspirin in tumor sites makes it promising as a new radiopharmaceutical for tumor imaging.