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

作者：Vidal Aurelien^*; Gaumet Vincent; Galmier Marie Josephe; Besse Sophie; Leal Fernand; Gachon Francoise; Viot Gilles; Metin Jacques; Chezal Jean Michel; Miot Noirault Elisabeth; Auzeloux Philippe

来源：Applied Radiation and Isotopes, 2015, 101: 1-9.

DOI：10.1016/j.apradiso.2015.03.010

• Kit formulation
• Freeze-drying
• Radiolabeling
• Technetium-99 m
• SPECT
• Proteoglycans imaging

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.

• 出版日期2015-7