131 I-trazodone: preparation, quality control and in vivo biodistribution study by intranasal and intravenous routes as a hopeful brain imaging radiopharmaceutical
| Autor: | M.E. Sayyed, I.T. Ibrahim, G. A. S. Awad, M. A. Motaleb |
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| Rok vydání: | 2017 |
| Předmět: |
Biodistribution
Hydrochloride Pharmacology 010403 inorganic & nuclear chemistry 030226 pharmacology & pharmacy 01 natural sciences High-performance liquid chromatography 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Labelling medicine Radiology Nuclear Medicine and imaging General Environmental Science business.industry General Engineering Trazodone In vitro 0104 chemical sciences Paper chromatography chemistry Anesthesia General Earth and Planetary Sciences Nasal administration business medicine.drug |
| Zdroj: | Revista Española de Medicina Nuclear e Imagen Molecular (English Edition). 36:371-376 |
| ISSN: | 2253-8089 |
| DOI: | 10.1016/j.remnie.2017.09.006 |
| Popis: | Objectives The preparation of 131I-trazodone hydrochloride and its biological evaluation as a promising brain imaging radiopharmaceutical using two routes of administration. Material and methods Trazodone (TZ) was radiolabelled with 131I using direct electrophilic substitution, and different factors affecting labelling yield were studied. Quality control of 131I-TZ was carried out using ascending paper chromatography, paper electrophoresis, and high pressure liquid chromatography (HPLC). In vivo biodistribution of 131I-TZ was evaluated in Swiss albino mice using 3 methods: intravenous 131I-TZ solution (IVS), intranasal 131I-TZ solution (INS), and intranasal 131I-TZ microemulsion (INME). Results Optimum labelling yield of 91.23 ± 2.12% was obtained with in vitro stability of 131I-TZ up to 6 h at room temperature. The biodistribution results showed a notably higher and sustained brain uptake for INME compared to IVS and INS at all time intervals. In addition, heart and blood uptake levels for INME were lower than those for IV solution which, in turn, could decrease the systemic side effects of trazodone. Also, the 131I-trazodone INME brain uptake of 6.7 ± 0.5%ID/g was higher than that of 99mTc-ECD and 99mTc-HMPAO (radiopharmaceuticals currently used for brain imaging). Conclusion 131/123I-trazodone formulated as INME could be used as a promising radiopharmaceutical for brain imaging. |
| Databáze: | OpenAIRE |
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