Nuclear Techniques ›› 2015, Vol. 38 ›› Issue (7): 70301-070301.doi: 10.11889/j.0253-3219.2015.hjs.38.070301

• NUCLEAR CHEMISTRY, RADIOCHEMISTRY, RADIOPHARMACEUTICALS AND NUCLEAR MEDICINE • Previous Articles     Next Articles

Comparison study of two 18F labeling methods of peptides

JIANG Dawei1 SUN Yanhong1 WANG Lihua1 LI Jianbo2 ZHANG Lan1   

  1. 1(Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Jiading Campus, Shanghai 201800, China) 2(Department of Nuclear Medicine, Inner Mongolia Medical University Affiliated Hospital, Hohhot 010050, China)
  • Received:2015-03-10 Revised:2015-04-10 Online:2015-07-10 Published:2015-07-10

Abstract: 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.

Key words: 18F, Radiolabeling of peptides, [18F]SFB, Al[18F]-NOTA