Lanreotide and octreotide complexed with technetium-99m: labeling, stability and biodistribution studies

Abstract

Lanreotide and Octreotide are cyclic octapeptide analogues of somatostatin that were labeled with the radioisotope Technetium-99m for use in diagnostic nuclear medicine. The peptides were processed in a tartrate/phthalate buffer solution containing reducing agent. The purpose of this investigation was to optimize direct labeling by varying some parameters, and to evaluate radiochemical stability and biodistribution in animals. The marked peptides were obtained with high labeling efficiency and no need for subsequent purification. Best radiolabeling results corresponded to a molar ratio of SnCl2.H2O/peptide of 4.5. 99mTc-peptides were radiochemically stable for 6 hours. 99mTc-octreotide was relatively more susceptible to cysteine challenge than 99mTc-lanreotide. 99mTc-peptides were mainly distributed in the gastrointestinal tract but 99mTc-lanreotide showed a greater uptake by the liver than 99mTc-octreotide. Results indicated that the products can be obtained with high radiochemical yield, in a simple routine appropriate for further studies to assess their efficacy in radiodiagnosis.