The case for fractional solubility profiles

This work reports the synthesis, radiolabeling and preliminary biodistribution results in tumor-bearing mice of ^99mTc(CO)₃(PA-TZ-CHC)]⁺. The novel colchicine (CHC) ligand was successfully synthesized via “click” reaction. Radiolabeling was performed in high yield with ^99mTc(CO)₃]⁺ core to get ^99mTc(CO)₃(PA-TZ-CHC)]⁺, which was hydrophilic and cationic, and was stable at room temperature. Biodistribution studies in tumor-bearing mice showed that ^99mTc(CO)₃(PA-TZ-CHC)]⁺ accumulated in the tumor with good uptake while comparatively low retention. The clearance of the ^99mTc-complex from normal organs was fast, resulting in increasing tumor/blood and tumor/muscle ratios. The promising results in preliminary biodistribution studies warrant further research to improve tumor targeting efficacy and pharmacokinetic profile of radiolabeled CHC derivative by structural modification.