Premium
Technetium‐99 m labeling and evaluation of olsalazine: a novel agent for ulcerative colitis imaging
Author(s) -
ElKawy O. A.,
Ibrahim I. T.,
Farah K.
Publication year - 2015
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3306
Subject(s) - chemistry , ulcerative colitis , biodistribution , technetium 99m , technetium , clearance , imaging agent , tracer , colitis , in vitro , scintigraphy , nuclear medicine , medicine , in vivo , nuclear chemistry , biochemistry , disease , urology , physics , microbiology and biotechnology , biology , nuclear physics
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.