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Background: Radiolabeled compounds can serve as diagnostic or therapeutic agents depending on the characteristics of the isotopes used. IMPY (6-iodo-2-(4′-dimethylamino)-phenyl-imidazo[1,2-a]pyridine) is a lipophilic derivative of thioflavin-T, designed to function as a tracer when labeled with radioactive iodine. While it has been primarily studied for imaging applications, its potential therapeutic effects when labeled with iodine-125 ([sup.125] I) remain to be explored. Methods: In this study, IMPY was synthesized and labeled with [sup.125] I for therapeutic purposes. Three different labeling methods were employed: isotope exchange reaction, redox reaction, and the Iodogen technique. The radiochemical yield of each method was determined to identify the most effective approach. Additionally, the effects of [sup.125] I-IMPY on neuroblastoma cells were evaluated by assessing its toxicity and cellular uptake. Results: The radiochemical yields for the isotope exchange reaction, redox reaction, and Iodogen technique were found to be 0.96%, 10.74%, and 96.52%, respectively. The Iodogen technique exhibited the highest yield, exceeding 90% even after 48 h, making it the most efficient method. Furthermore, the impact of [sup.125] I-IMPY on neuroblastoma cells was analyzed, revealing significant cellular uptake and potential therapeutic effects. Conclusions: This study demonstrated that the Iodogen technique is the most effective method for labeling IMPY with [sup.125] I. The high labeling efficiency and observed cellular effects suggest that [sup.125] I-IMPY could be considered not only as a tracer but also as a potential therapeutic agent for neuroblastoma. Further studies are needed to explore its full therapeutic potential and mechanism of action.

Background: Radiolabeled compounds can serve as diagnostic or therapeutic agents depending on the characteristics of the isotopes used. IMPY (6-iodo-2-(4′-dimethylamino)-phenyl-imidazo[1,2-a]pyridine) is a lipophilic derivative of thioflavin-T, designed to function as a tracer when labeled with radioactive iodine. While it has been primarily studied for imaging applications, its potential therapeutic effects when labeled with iodine-125 (125I) remain to be explored. Methods: In this study, IMPY was synthesized and labeled with 125I for therapeutic purposes. Three different labeling methods were employed: isotope exchange reaction, redox reaction, and the Iodogen technique. The radiochemical yield of each method was determined to identify the most effective approach. Additionally, the effects of 125I-IMPY on neuroblastoma cells were evaluated by assessing its toxicity and cellular uptake. Results: The radiochemical yields for the isotope exchange reaction, redox reaction, and Iodogen technique were found to be 0.96%, 10.74%, and 96.52%, respectively. The Iodogen technique exhibited the highest yield, exceeding 90% even after 48 h, making it the most efficient method. Furthermore, the impact of 125I-IMPY on neuroblastoma cells was analyzed, revealing significant cellular uptake and potential therapeutic effects. Conclusions: This study demonstrated that the Iodogen technique is the most effective method for labeling IMPY with 125I. The high labeling efficiency and observed cellular effects suggest that 125I-IMPY could be considered not only as a tracer but also as a potential therapeutic agent for neuroblastoma. Further studies are needed to explore its full therapeutic potential and mechanism of action.

Background Inflammation serves as a natural defense mechanism; however, its persistence can lead to chronic diseases with serious clinical consequences. Early detection of inflammation is therefore critical to slowing disease progression and improving therapeutic outcomes. Methods In this study, cefaclor (Cefa) was successfully radiolabeled with iodine-131 via electrophilic substitution to facilitate the detection of infected and inflamed muscles in mouse models. The labeling reaction was carried out with 100 µg of Cefa and 100 µg of iodogen, using glass frits as the oxidizing system at pH 7 and 60 °C, with 10 µL of Na 131 I for 20 min. The resulting [ 131 I]Cefa was purified by high-performance liquid chromatography (HPLC). Molecular modeling was performed in the Molecular Operating Environment (MOE) to evaluate the compound’s structure and binding affinity. Results The labeling process was optimized to achieve a radiolabeling efficiency of 90 ± 0.56%, and stability of about 89 ± 0.5% at 4 h. Docking simulations confirmed strong binding of [ 131 I]Cefa to bacterial DNA gyrase B, supporting its potential as a targeted imaging agent. Biological evaluation in mouse models demonstrated notable tracer accumulation in both septic and sterile inflammatory sites. Uptake values reached 28 ± 1.5%ID/organ in infected muscles and 16 ± 1.5%ID/organ in sterile inflammation at 120 minutes post-injection. The target-to-non-target (T/NT) ratios were 5.28 for infected muscles and 2.1 for sterile inflammation, indicating effective differentiation between bacterial (septic) and non-bacterial (aseptic) inflammatory foci. Conclusion The radiolabeled [ 131 I]Cefa compound exhibits promising diagnostic capabilities for distinguishing bacterial infections from sterile inflammation. Its high radiolabeling efficiency, strong molecular binding, and selective in vivo uptake support its potential utility as a non-invasive imaging agent for early detection and characterization of inflammatory conditions. Highlights Objective: To develop a radiolabeled cefaclor compound ([ 1 3 1 I] Cefa) for early imaging and differentiation between bacterial infections and sterile inflammation. Radiolabeling Method: Cefaclor was labeled with iodine-131 via electrophilic substitution, achieving a high radiochemical yield of 90 ± 0.56% using iodogen and glass frits as the oxidizing system. Structural Analysis: Molecular modeling and docking simulations confirmed strong binding of [ 1 3 1 I] Cefa to bacterial DNA gyrase B, supporting its role as a targeted imaging agent. In Vivo Findings: In mouse models, the compound showed significant uptake in infected (28± 1.5%) and sterile inflamed tissues (16 ± 1.5%) at 120 minutes post-injection. Diagnostic Value: The target-to-non-target ratios (28 for infection, 2.1 for sterile inflammation) demonstrate the compound’s potential to distinguish between infectious and non-infectious inflammation.

The application of nanomaterials in the treatment of various types of diseases continues to increase, including the use of silver nanoparticles (AgNPs). However, there still limitation in terms of the research on labelling AgNPs using radioactive compound such as 131I. The aim of this study is to carry out a method on 131I radiolabelling of AgNPs by using Iodogen as an iodination reagent. The radiolabelled 131I-AgNPs were then purified by using Sephadex-25 column chromatography with 0,05 M phosphate buffer solution as mobile phase for the first purification and HEPES solution for the second purification. The radiochemical purity of radiolabelled 131I-AgNPs was then determined by using autoradiography scanner. 131I-AgNPs with a purity 94,5±0,2121% were obtained after the purification. Stability test of the 131I-AgNPs was carried out by determining the radiochemical purity of the 131I-AgNPs on the first day until the fifth day of storage in the room temperature and refrigerator. The best stability of the 131I-AgNPs after purification resulted in radiochemical purity >90% until the fourth day and <90% on the fifth and subsequent days in both storages. This result shows that storage in the refrigerator can be a better choice rather than in the room temperature.

The aim of this study was to develop a safe and simple radiolabeling and purification procedure for high-dose [sup.131]I-rituximab for treatment of patients with non-Hodgkin's lymphoma. As the starting point, the conventional Iodogen-coated vial method was applied. After the iodogen-coated monoclonal antibody (mAb) method, a labeling method involving much lower amounts of iodogen was assessed. Subsequently, [sup.131]I-rituximab was purified with a tangential flow filtration system. Quality control of the final product was performed by using size-exclusion chromatography with ultraviolet detection and by instant high-performance thin-layer chromatography. Immunoreactivity was determined by using a cell-binding assay. During the labeling procedure, radiation exposure was monitored. The coated vial method resulted in a low radiation exposure, but immunoreactivity was highly compromised (37%). Also, formation of aggregates was observed. The maximal observed effective dose was 18 µSv, finger thermoluminescence dosemeters revealed a hand-dose measurement of 0.8 mSv. The second method resulted in an immunoreactivity of 70%. Radiochemical purity was >97% after purification. The maximal measured effective dose was 31 µSv, and detected exposure to the hands was 1.9 mSv. We have developed a simple labeling technique for the preparation of high-dose [sup.131]I-rituximab. The method offers a high purity and retained immunoreactivity with minimal radiation exposure for involved personnel.