title: Development of a freeze-dried kit formulation for the preparation of 99mTc-NTP 15-5, a radiotracer for scintigraphic imaging of proteoglycans.
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.
authors: Inserm, UMR 990, F-63005 , France; Clermont Université, Université d'Auvergne, Imagerie moléculaire et thérapie vectorisée, BP 10448, F-63000 Clermont-Ferrand, France. Electronic address: aurelien.vidal@udamail.fr.
authors: Aurélien
authors: A
authors: Vidal
authors: Inserm, UMR 990, F-63005 , France; Clermont Université, Université d'Auvergne, Imagerie moléculaire et thérapie vectorisée, BP 10448, F-63000 Clermont-Ferrand, France.
authors: Vincent
authors: V
authors: Gaumet
authors: Inserm, UMR 990, F-63005 , France; Clermont Université, Université d'Auvergne, Imagerie moléculaire et thérapie vectorisée, BP 10448, F-63000 Clermont-Ferrand, France.
authors: Marie-Josèphe
authors: MJ
authors: Galmier
authors: Inserm, UMR 990, F-63005 , France; Clermont Université, Université d'Auvergne, Imagerie moléculaire et thérapie vectorisée, BP 10448, F-63000 Clermont-Ferrand, France.
authors: Sophie
authors: S
authors: Besse
authors: Inserm, UMR 990, F-63005 , France; Clermont Université, Université d'Auvergne, Imagerie moléculaire et thérapie vectorisée, BP 10448, F-63000 Clermont-Ferrand, France.
authors: Fernand
authors: F
authors: Leal
authors: Clermont Université, Université d'Auvergne, BP 10448, F-63000 Clermont-Ferrand, France; Department of nuclear medicine, Center Jean Perrin, F-63011 Clermont-Ferrand, France.
authors: Françoise
authors: F
authors: Gachon
authors: Laboratoires CYCLOPHARMA, Biopôle Clermont-Limagne, F-63360 Saint-Beauzire, France.
authors: Gilles
authors: G
authors: Viot
authors: Clermont Université, Université d'Auvergne, BP 10448, F-63000 Clermont-Ferrand, France.
authors: Jacques
authors: J
authors: Métin
authors: Inserm, UMR 990, F-63005 , France; Clermont Université, Université d'Auvergne, Imagerie moléculaire et thérapie vectorisée, BP 10448, F-63000 Clermont-Ferrand, France.
authors: Jean-Michel
authors: JM
authors: Chezal
authors: Inserm, UMR 990, F-63005 , France; Clermont Université, Université d'Auvergne, Imagerie moléculaire et thérapie vectorisée, BP 10448, F-63000 Clermont-Ferrand, France.
authors: Elisabeth
authors: E
authors: Miot-Noirault
authors: Inserm, UMR 990, F-63005 , France; Clermont Université, Université d'Auvergne, Imagerie moléculaire et thérapie vectorisée, BP 10448, F-63000 Clermont-Ferrand, France.
authors: Philippe
authors: P
authors: Auzeloux
mesh_terms: D000818:Animals; D002356:Cartilage / Q000000981:diagnostic imaging* / Q000378:metabolism*; D002357:Cartilage Diseases / Q000000981:diagnostic imaging / Q000378:metabolism; D002626:Chemistry, Pharmaceutical; D005612:Freeze Drying / Q000379:methods; D006573:Heterocyclic Compounds, 1-Ring / Q000097:blood / Q000302:isolation & purification* / Q000493:pharmacokinetics; D007202:Indicators and Reagents; D015609:Organotechnetium Compounds / Q000097:blood / Q000302:isolation & purification* / Q000493:pharmacokinetics; D011509:Proteoglycans / Q000378:metabolism*; D000644:Quaternary Ammonium Compounds / Q000097:blood / Q000302:isolation & purification* / Q000493:pharmacokinetics; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000097:blood / Q000302:isolation & purification* / Q000493:pharmacokinetics; D051381:Rats; D013667:Technetium / Q000097:blood / Q000302:isolation & purification* / Q000493:pharmacokinetics
chemical_list: D006573:Heterocyclic Compounds, 1-Ring; D007202:Indicators and Reagents; C407019:N-(triethylammonium)-3-propyl(15)ane-N5; D015609:Organotechnetium Compounds; D011509:Proteoglycans; D000644:Quaternary Ammonium Compounds; D019275:Radiopharmaceuticals; D013667:Technetium
keywords: Freeze-drying; Kit formulation; Proteoglycans imaging; Radiolabeling; SPECT; Technetium-99m