Development of (111)In-labeled porphyrins for SPECT imaging

OBJECTIVE(S): The aim of this research was the development of (111)In-labeled porphyrins as possible radiopharmaceuticals for the imaging of tumors. METHODS: Ligands, 5, 10, 15, 20-tetrakis (3, 5-dihydroxyphenyl) porphyrin) (TDHPP), 5, 10, 15, 20-tetrakis (4-hydroxyphenyl) porphyrin (THPP) and 5, 10, 15, 20-tetrakis (3,4-dimethoxyphenyl) porphyrin) (TDMPP) were labeled with (111)InCl3 (produced from proton bombardment of natCd target) in 60 min at 80 ºC. Quality control of labeled compounds was performed via RTLC and HPLC followed by stability studies in final formulation and presence of human serum at 37 ºC for 48 h as well as partition coefficient determination. The biodistribution studies performed using tissue dissection and SPECT imaging up to 24h. RESULTS: The complexes were prepared with more than 99% radiochemical purity (HPLC and RTLC) and high stability to 48 h. Partition coefficients (calculated as log P) for (111)In-TDHPP, (111)In-THPP and (111)In-TDMPP were 0.88, 0.8 and 1.63 respectively. CONCLUSION: Due to urinary excretion with fast clearance for (111)In-TDMPP, this complex is probably a suitable candidate for considering as a possible tumor imaging agent.