Radiochemical and biological characteristics of radioactive iodine labeled indomethacin for imaging of inflammation

Summary

Indomethacin was successfully labeled with ¹²⁵I. This labeling reaction was carried out via electrophilic substitution of hydrogen atom with the iodonium atom I⁺. The reaction was found to be strongly dependent on pH of the reaction medium. At neutral pH value, 7 the labeling yield was maximum. This may be due to the good solubility of indomethacin, good protonation and good working of the oxidizing agent at this pH value. Towards the acidic pH value, the yield decreased and towards the alkaline pH value the yield decreased due to the decomposition of the indomethacin. The labeling reaction is very fast but needs five minutes for completion. The produced ¹²⁵I-indomethacin was found stable in-vivo as the thyroid gland uptake did not exceed 2%. Labeled indomethacin shows a good localization in inflamed muscle, either septic or sterile. It excretes mainly via liver and to some extent via kidney. The imaging must be carried out at 24-hour post injection, after that time, the background activity has cleared and the activity is concentrated in the target site.