Preparation and evaluation of radiolabeled acetaminosalol microspheres: A new potential selective radiotracer for ulcerative colitis early diagnosis

In this study,99mTc- acetaminosalol was developed, characterized, and formulated as pH-sensitive microspheres. The preliminary preclinical qualifications of the formulated radiopharmaceutical were assessed in silico, in vitro, and in vivo. Overall, the reported data encouraged the potential use of the labeled microspheres to target ulcerative colitis. Acetaminosalol labeling reaction with technetium-99m was optimized, and the radiocomplex was obtained in a high radiochemical yield of 98.9  ± 0.6% and high stability (>30  h). The tracer was characterized, and its binding to the PPARγ receptor was assessed in silico. To reduce radiation exposure to non-target organs and increase accumulation in the colon, the tracer was formulated as pH-sensitive microspheres with a mean particle size of 201 ± 2.1 μm, a pol ydispersity index of 0.18, a 25.3 ± 3.6 zeta potential, and 98.6 ± 0.33% entrapment efficiency. The system suitability was assessed in vivo in normal and ulcerative rats, and the biodistribution profile in the colon showed 56.5 ± 1.4% localization within 4 h. Blocking study suggested the selectivity of the tracer to the target receptor. Overall, the reported data encouraged the potential use of the labeled microspheres to target ulcerative colitis.
Source: Journal of Labelled Compounds and Radiopharmaceuticals - Category: Biochemistry Authors: Tags: RESEARCH ARTICLE Source Type: research