Development of a freeze-dried kit formulation for the preparation of 99mTc-NTP 15-5, a radiotracer for scintigraphic imaging of proteoglycans. (July 2015)

• Record Type: Journal Article
• Authors: Vidal, Aurélien; Gaumet, Vincent; Galmier, Marie-Josèphe; Besse, Sophie; Leal, Fernand; Gachon, Françoise; Viot, Gilles; Métin, Jacques; Chezal, Jean-Michel; Miot-Noirault, Elisabeth; Auzeloux, Philippe
• Is Part Of: Applied radiation and isotopes. Volume 101(2015:Jul.)
• Page Start: 1
• Page End: 9
• Publication Date: 2015-07
• Subjects: Kit formulation -- Freeze-drying -- Radiolabeling -- Technetium-99 m -- SPECT -- Proteoglycans imaging; Radiology -- Periodicals; Radiation -- Industrial applications -- Periodicals; Nuclear chemistry -- Periodicals; Internet resource; Periodical; 660.298
• DOI: 10.1016/j.apradiso.2015.03.010
• Languages: English
• ISSNs: 0969-8043

Abstract

Abstract: 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. 99m Tc-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 99m Tc-NTP 15-5 (radiochemical yields 94.6±1.8%). 99m Tc-NTP 15-5 was stable and resulted in favorable biological evaluations. Highlights: Synthesis and radiolabeling of 99m Tc-NTP 15-5. A lyophilized kit was successfully developed for preparation of 99m Tc-NTP 15-5. High storage stability of NTP 15-5 kit. 99m Tc-NTP 15-5 resulted in favorable biological evaluations.