[Tumor targeting efficacy of a novel PET radiotracer (1)8F-AlF-NOTA-PRGD2 in mice].
OBJECTIVE
To investigate the tumor targeting efficacy of (18)F-AlF-NOTA-PRGD2, a novel radiotracer of Arginine-glycine-aspartic acid (RGD) peptides.


METHODS
(18)F-AlF-NOTA-PRGD2 was synthesized in one-step by conjugating NOTA-PRGD2 with (18)F-AlF at 100 degrees celsius;. The tumor targeting efficacy and in vivo biodistribution profile of (18)F-AlF-NOTA-PRGD2, following intravenous injection via the tail vein, were evaluated in a nude mouse model bearing subcutaneous U87MG glioblastoma xenograft by radioactivity biodistribution assessment, PET/CT and microPET/CT.


RESULTS
NOTA-PRGD2 was (18)F-fluorinated successfully in one-step with a yield of 17%-25% within 15-20 min. Radioactivity biodistribution study confirmed the tumor-targeting ability of (18)F-AlF-NOTA-PRGD2 in the tumor-bearing mice. At 1 and 2 h following injection, (18)F-AlF-NOTA-PRGD2 uptake in the tumor reached 4.14∓1.44 and 2.80∓1.18 % ID/g (t=1.910, P=0.070) with tumor/brain ratios of 2.95∓0.61 and 5.21∓2.62, respectively (t=-1.686, P=0.167). Both PET/CT and microPET/CT were capable of showing the radioactivity biodistribution of (18)F-AlF-NOTA-PRGD2 in the mouse model and clearly displayed the tumor, but microPET/CT showed a much better image quality.


CONCLUSIONS
(18)F-AlF-NOTA-PRGD2 prepared by one-step radiosynthesis can selectively target to the tumor, demonstrating its potential as a good radiotracer for tumor imaging.
PET Center, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China. E-mail: wuhbym@tom.com.
Hubing
H
Wu
Quanshi
Q
Wang
Yanjiang
Y
Han
Wenlan
W
Zhou
Hongsheng
H
Li
Ying
Y
Tian
Qiaoyu
Q
Wang
D000818:Animals; D045744:Cell Line, Tumor; D005462:Fluorine Radioisotopes; D005909:Glioblastoma / Q000000981:diagnostic imaging*; D006801:Humans; D051379:Mice; D008819:Mice, Nude; D009842:Oligopeptides; D049268:Positron-Emission Tomography / Q000379:methods*; D011849:Radioactive Tracers
D005462:Fluorine Radioisotopes; D009842:Oligopeptides; D011849:Radioactive Tracers; C047981:arginyl-glycyl-aspartic acid