title: Technetium-99 m labeling and evaluation of olsalazine: a novel agent for ulcerative colitis imaging.
abstract: Ulcerative colitis is a chronic disease having a regressive nature. Commonly used diagnostic methods have the disadvantage to be invasive, time-consuming, and expensive. Therefore, a new sensitive method for the detection and monitoring of disease activity is urgently needed in clinical practice. In the current investigation, radio complexation of olsalazine with technetium-99m, its characterization, and optimization of the labeling conditions were explored. Optimum radiochemical yield of (99m) Tc-olsalazine (97.6% ± 1.8%) was obtained via direct complexation with technetium-99m (~200 MBq) in the presence of stannous chloride dihydrate (100 µg) as reducing agent at pH 6. It was observed that the complex showed significant in vitro stability in serum at 37°C for more than 11 h. The computer-generated optimized geometries of the (99m) Tc-olsalazine were reported, and biodistribution studies were carried out using chemically and microbiologically mice-induced ulcerative colitis models. The tracer showed a good localization in both models and was excreted mainly via liver and to some extent via kidney. Imaging can be performed at 1-2 h post-injection; at that time, the background activity has cleared, and the activity is concentrated in the target site. All the gathered biological data supported the usefulness of (99m) Tc-olsalazine as a potential imaging agent for ulcerative colitis.
authors.affiliation: Atomic Energy Authority, Cairo, Egypt.
authors.forename: O A
authors.initials: OA
authors.lastname: El-Kawy
authors.affiliation: Atomic Energy Authority, Cairo, Egypt.
authors.forename: I T
authors.initials: IT
authors.lastname: Ibrahim
authors.affiliation: Atomic Energy Authority, Cairo, Egypt.
authors.forename: K
authors.initials: K
authors.lastname: Farah
mesh_terms: D000636:Aminosalicylic Acids / Q000737:chemistry / Q000493:pharmacokinetics*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry / Q000493:pharmacokinetics*; D003093:Colitis, Ulcerative / Q000000981:diagnostic imaging* / Q000378:metabolism / Q000473:pathology*; D007091:Image Processing, Computer-Assisted / Q000379:methods*; D007553:Isotope Labeling / Q000379:methods; D051379:Mice; D015609:Organotechnetium Compounds / Q000737:chemistry / Q000493:pharmacokinetics*; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000737:chemistry / Q000493:pharmacokinetics*; D014018:Tissue Distribution
chemical_list: D000636:Aminosalicylic Acids; D000894:Anti-Inflammatory Agents, Non-Steroidal; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; C032587:olsalazine
keywords: in vivo evaluation; olsalazine; technetium-99m; ulcerative colitis imaging