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Development of a complementary PET/MR dual-modal imaging probe for targeting prostate-specific membrane antigen (PSMA)

Published: 2017-01-11

Keyword: Encapsulation,GUL,Prostate cancer,Multi-modal,Gallium-68

 Literature  Nanomedicine, IF 4.889


Background & Purpose Prostate cancer is one of the most common types of cancer in the world. The prostate specific membrane antigen (PSMA) is a famous biomarker of prostate cancer, and the glutamate-urea-lysine (GUL) conjugate is a proven PSMA targeting moiety. Iron oxide (IO) nanoparticle is for MRI imaging and 68Ga-DOTA is for PET positron emission. 68Ga-DOTA, GUL, PEG are all encapsulated in 68Ga-DOTA-IO-GUL imaging probe, of which selective uptake by PSMA+ tumor is demonstrated. Specific binding of DOTA-IO-GUL to PSMA-positive cells was confirmed by an in vitro competitive binding study using PSMA-targeting agent MIP-1072.



Fig.1 In vivo micro MRI image results. (A) Before injection, control image; (B) after injection of DOTA-IO-GUL (0.1 mL, 0.2 mM) through the tail vein (1 h). Left tumor is PSMA positive (22Rv1) and right tumor is PSMA-negative (PC-3). Red circle demonstrates the selective uptake of DOTA-IO-GUL to the positive tumor (49.1 Fe ng/g).



Fig. 2 In vivo PET result. (A) PSMA-selective uptake result in micro PET imaging. (SUVmean = 0.668) 68Ga-DOTA-IO-GUL (10.2 MBq, 0.1 mL) tail vein injection after 1 h imaging. Left tumor is PSMA-positive (22Rv1) and right tumor is PSMA-negative (PC-3). (B) Blocking study result with co-injection of MIP-1072 (50 mg/kg).