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Avanafil was labeled with technetium-99m for diagnostic evaluation of erectile dysfunction. The labeling conditions were optimized to reach a high radiolabeling yield (98.6%). The complex showed good stability for up to 24 h in saline and 20 h in serum. The structure of the labeled complex was confirmed. Molecular modeling and docking to the PDE5 enzyme were performed to evaluate the complex fitting and binding to its biochemical target. Biodistribution in normal rats and three different models of erectile dysfunction were performed. The results strongly suggest that 99mTc-avanafil is a promising tracer for erectile dysfunction in humans. [ABSTRACT FROM AUTHOR]

Antineoplastons (ANPs) are compounds that have antitumor activities. ANPA10 was labeled with technetium-99m using stannous chloride as a reducing agent with the labeling yield of approximately 98% at pH 6. The conditions required to optimize the labeling yield were studied in details. The tumor binding specificity of the [99mTc]Tc-ANPA10 radiotracer was evaluated. The uptake of [99mTc]Tc-ANPA10 in ascitic fluid uptake was 10, 16, and 12.8% ID/g at 30, 60, and 120 min post injection. The preclinical biological evaluation of [99mTc]Tc-ANPA10 complex in solid tumor bearing mice showed a high tumor uptake at 1 h post injection (11.2 ± 0.30 % ID/g). The selective uptake of [99mTc]Tc-ANPA10 in solid tumors and rapid clearance from nontarget organs make it promising for solid tumor imaging, but further clinical trials are required. [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]

Brain abscess is a life-threatening condition that requires a timely and accurate diagnosis. In this study, linezolid, an oxazolidinone antibiotic, was labeled with technetium-99m according to the stannous chloride method. The labeling reaction factors were studied and optimized to achieve a high yield (97.4 ± 2.3%). The 99m Tc-linezolid was radio- and physico-chemically characterized to assess its suitability as a radiopharmaceutical for the brain. In-silico docking to target peptidyltransferase showed an optimal binding fit (energy = -66.6 Kcal/mol). The complex was biologically evaluated in-vitro using binding assays in alive and heat-killed bacteria and in-vivo in an MRSA brain infection model. All results suggested that the labeled complex could potentially be a new nuclear imaging agent to diagnose and localize brain abscesses specifically., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2023 Elsevier Ltd. All rights reserved.)

Brain cancer is a challenging disease to treat using conventional approaches. The present investigation aimed to develop a radiopharmaceutical targeting brain cancer based on natural isovanillin. Different parameters were optimized, resulting in high radiolabeling efficiency (97.3 ± 1.2%) and good stability (<48 h). The tracer was formulated for intranasal delivery in a chitosan nanoparticles system with a mean particle size of 141 ± 2 nm, a polydispersity index of 0.23 ± 0.02, and a zeta potential of -17.4 ± 0.3 mV to enhance nasal uptake and surmount the blood-brain barrier. The system was characterized and assessed in-vitro for suitability and specificity and evaluated in-vivo in normal and tumorized mice. The biodistribution profile in brain tumor showed 20.5 ± 0.4 %ID/g localization and cancer cell targeting within 60 min. Improvement in brain tumor uptake resulted from both the nanoformulation and nasal administration of iodoisovanillin. Overall, the reported results encourage the potential use of the nanoformulated labeled compound as an anticancer agent., Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper., (Copyright © 2022 Elsevier Ltd. All rights reserved.)