Abstract
Objective To prepare a novel radiolabeled FR-positive tumor targeting agent 99Tcm-(HYNIC-NHHN-FA) (EDDA) and evaluate its biological properties. Methods FA derivative FA-NHHN-HYNIC was synthesized and radiolabeled with 99Tcm using EDDA as a coligand. The radiochemical purity, octanal/water partition coefficient and in vitro stabilities of the complex were studied after purified by HPLC. In vitro cellular uptakes were performed on FR-positive KB cells (human oral epidermoid carcinoma cells). Biodistribution and microSPECT/CT imaging were investigated on normal Kunming mice and nude mice bearing KB tumors, respectively. Results The radiochemical purity of the complex was over 95% after purified by HPLC. It displayed high stability both in saline and in serum. It also exhibited high specific FR binding in FR-positive KB cells in vitro. The binding ratio was (6.76±0.60)% 1 h after incubation, and decreased to (0.24±0.02)% after adding excessive FA. The results of biodistribution showed high kidney uptake in normal mice, and the uptake reached (21.79±9.79) %ID/g 0.5 h after injection. Flank KB tumors were clearly visualized with 99Tcm-(HYNIC-NHHN-FA)(EDDA) by microSPECT/CT imaging at 2 h postinjection, and the uptake could be inhibited by excessive FA. Conclusions 99Tcm-(HYNIC-NHHN-FA)(EDDA) exhibits good pharmacokinetic properties, suggesting its potential as a promising FA targeting agent for tumor imaging. Key words: Folic acid; Isotope labeling; Technetium; Carcinoma; Tomography, emission-computed, single-photon; Tomography, X-ray computed; Mice
Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
