title: Influence of technetium-99m-labeling conditions on physico-chemical and related biological properties of an acylated poly-galactosidic macrophage targeting agent for inflammation imaging.
abstract: The potential of 99m-Tc-J001 for the investigation of inflammatory lesions via the targeting of recruited macrophages (M phi) has already been documented in several experimental models and in human diseases. To achieve a functional imaging of inflammation via M phi targeting, minimal labeled colloid content and high in vivo stability of 99mTc-J001 are essential. The actual specificity of such scintigraphy is closely dependent upon the radiolabeling of only the J001 molecules available for M phi targeting. To develop an appropriate radiopharmaceutical kit, optimization of the labeling conditions was achieved from a series of pilot formulations that were evaluated for radiolabeling efficiency and both in vitro and in vivo 99mTc-J001 stability. Colloids were characterized using autocorrelation spectroscopy and multiangle laser-light scattering, radioactive colloid content of the formulations being deduced from biodistribution studies. This work has made possible the definition of a formulation exhibiting a radiolabeling yield > 97.0%, associated with in vivo stability and minimal colloid formation, thus greatly enhancing the specificity of such macrophage scintigraphy.
authors.affiliation: Laboratoire de Biophysique Cellulaire et RMN, INSERM U316-CNRS, Faculté de Médecine, Tours, France.
authors.forename: F
authors.initials: F
authors.lastname: Perin
authors.forename: L
authors.initials: L
authors.lastname: Routledge
authors.forename: O
authors.initials: O
authors.lastname: N'Doye
authors.forename: M
authors.initials: M
authors.lastname: M'Bodj
authors.forename: G
authors.initials: G
authors.lastname: Normier
authors.forename: A
authors.initials: A
authors.lastname: Le Pape
mesh_terms: D000818:Animals; D001168:Arthritis / Q000000981:diagnostic imaging; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004355:Drug Stability; D006017:Glycolipids / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D007249:Inflammation / Q000000981:diagnostic imaging* / Q000473:pathology*; D007553:Isotope Labeling / Q000379:methods; D008264:Macrophages / Q000000981:diagnostic imaging*; D009682:Magnetic Resonance Spectroscopy / Q000379:methods; D008297:Male; D015609:Organotechnetium Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D010758:Phosphorus; D011817:Rabbits; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar; D014018:Tissue Distribution
chemical_list: D006017:Glycolipids; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; C098281:technetium Tc 99m J001X; D010758:Phosphorus