Development of a freeze-dried kit formulation for the preparation of Tc-99m-NTP 15-5, a radiotracer for scintigraphic imaging of proteoglycans

摘要

The cartilage-targeting strategy is based on the strong affinity of quaternary ammonium (QA) functions for cartilage proteoglycans. We use a bifunctional agent containing QA moiety and a polyazamacrocycle structure able to complex technetium-99m. Tc-99m-NTP 15-5 was selected for its high stability and its high affinity for proteoglycans in vivo. Labeling conditions of NTP 15-5 were optimized, and a lyophilized kit was developed for radiolabeling of Tc-99m-NTP 15-5 (radiochemical yields 94.6 +/- 1.8%). Tc-99m-NTP 15-5 was stable and resulted in favorable biological evaluations. (C) 2015 Elsevier Ltd. All rights reserved.