Synthesis, characterization and evaluation of 99Tc/99mTc DIARS and DMPE complexes containing pentadecanoic acid

The synthesis and purification of two new ligands, 15-[bis(3,4-dimethyl arsino)phenyl] pentadecanoic acid (FA-DIARS) and [bis(16,17-dimethyl phosphino)] heptadecanoic acid (FA-DMPE) and the preparation of their corresponding 99Tc/99mTc complexes of the general formula [Tc(III)L2Cl2]+, wherein L is FA-DIARS or FA-DMPE are reported. After careful purification by preparative HPLC, the 99Tc complexes were characterized by spectroscopy, while the 99mTc complexes were used to determine the biodistribution in mice. The results of the organ distribution studies indicated a relatively high uptake in heart (5-7% dose/g). The complexes were, however, found to be very slowly cleared from the blood, probably due to strong binding to serum proteins. Further, the heart to liver and heart to lung ratios were unfavourable. Attempts to improve the efficacy by synthesizing complexes containing one fatty acid per molecule are also described.