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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 polydispersity 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. [ABSTRACT FROM AUTHOR]

About 35% reduction in cancer deaths among patients having solid tumors is related to using aspirin, which encouraged us to develop a new specific tumor diagnostic radiopharmaceutical agent. This can be done by direct labeling of aspirin with technetium-99m using stannous chloride as a reductant at pH 9. At this pH, aspirin is saponificated to salicylate ions. Salicylate binds to pertechenetate to form 99mTc salicylate complex. The radiochemical yield (RCY, %) of 99mTc-salicylate complex obtained from aspirin was determined using paper chromatography, electrophoresis, and HPLC and was found to reach 90.2%. The 99mTc salicylate complex obtained from aspirin was stable for up to 5 h. The tumor uptake of the 99mTc salicylate complex obtained from aspirin was determined by ex-vivo study in tumor-bearing mice. This study showed that 99mTc salicylate complex was concentrated in tumor sites (ascites or solid), allowing tumor radioimaging. High target/non-target (tumor muscles/normal muscles) uptake ratio shows that 99mTc salicylate complex can be utilized for early detection of solid tumors. Molecular modeling and docking study conofirm the possibility of using the radiolabeled 99mTc salicylate complex for specific cancer imaging in binding with epidermal growth factor receptors (EGFR). [ABSTRACT FROM AUTHOR]