Background: Some radiopharmaceuticals based on peptides have been applied in preclinical and clinical trials

in the meantime

a large number of peptides are to be exploited. After years of development

radiolabeling techniques of peptides have progressed to be a system method. Through these methods of radiolabeling

peptides’ physiological activities would be influenced. Purpose: In this paper

we summarized two current commonly used 18F labeling methods for preparation of radiopharmaceuticals based on peptides. Methods: By comparison of labeling conditions

radiochemistry yields

specific activity of labeling products

radiochemistry purity

stability and pharmacokinetics of final products

we evaluated advantages and disadvantages of the two methods

with the hope to provide reference data for future research of 18F-labeled peptide radiopharmaceuticals. Results: Both [18F]SFB and Al18F-NOTA could readily label RGDyk peptide with 18F

with a radiochemistry yield of about 8.5% and 15%

respectively. [18F]SFB could produce radiolabeled peptides with better specific activity

while Al18F-NOTA proved to be a more time-saving method. For stability test

more than 80% of both [18F]SFB and Al18F-NOTA could maintain intact in PBS (Phosphate Buffer Solution) or BSA (Bovine Serum Albumin) within 360 min

and about 50% radiolabeled peptides could survive in vivo. Conclusion: The in vitro and in vivo stability of [18F]-RGD obtained with both methods were excellent

and biodistribution pattern of radiolabeled products via two methods did not show obvious differences. Abstract