The possibility of a fully automated procedure for radiosynthesis of fluorine-18-labeled fluoromisonidazole using a simplified single,neutral alumina column purification procedure |
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| Authors: | Saikat Nandy M.G.R. Rajan A. Korde N.V. Krishnamurthy |
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| Affiliation: | 1. Radiation Medicine Centre, Bio-Medical Group, Bhabha Atomic Research Centre, Tata Memorial Hospital Annexe, Parel, Mumbai-400 012, India;2. Radiopharmaceuticals Division, Radiochemistry & Isotope Group, Bhabha Atomic Research Centre, Trombay, Mumbai-400 085, India;3. Medical Cyclotron Facility, Board of Radiation and Isotope Technology, Department of Atomic Energy, Tata Memorial Hospital Annexe, Parel, Mumbai-400 012, India;1. Department of Medicine, Rheumatology Division, Calcutta Medical College, Kolkata;2. Department of Preventive and Social Medicine, All India Institute of Hygiene and Public Health, Kolkata, India;3. Department of Microbiology, GSL Medical College, Rajahmundry, AP, India;2. Department of Radiation Oncology, University of Washington, Seattle, WA;1. Department of Electrical Engineering, National Institute of Technology, Agartala, Barjala, Jirania, Tripura (West), 799046, India;2. Department of Chemical Engineering, National Institute of Technology, Agartala, Barjala, Jirania, Tripura (West), 799046, India;2. CSIRO Computational Informatics, The Australian e-Health Research Centre, Herston, Queensland, Australia;3. School of Medicine, University of Queensland, St Lucia, Brisbane, Queensland, Australia;4. Department of Radiation Oncology, Royal Brisbane and Women’s Hospital, Herston, Brisbane, Queensland, Australia;5. Australian Institute for Bioengineering and Nanotechnology, The University of Queensland, St Lucia, Brisbane, Queensland, Australia |
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| Abstract: | A novel fully automated radiosynthesis procedure for [18F]Fluoromisonidazole using a simple alumina cartridge-column for purification instead of conventionally used semi-preparative HPLC was developed. [18F]FMISO was prepared via a one-pot, two-step synthesis procedure using a modified nuclear interface synthesis module. Nucleophilic fluorination of the precursor molecule 1-(2′-nitro-1′-imidazolyl)-2-O-tetrahydropyranyl-3-O-toluenesulphonylpropanediol (NITTP) with no-carrier added [18F]fluoride followed by hydrolysis of the protecting group with 1 M HCl. Purification was carried out using a single neutral alumina cartridge-column instead of semi-preparative HPLC. The maximum overall radiochemical yield obtained was 37.49±1.68% with 10 mg NITTP (n=3, without any decay correction) and the total synthesis time was 40±1 min. The radiochemical purity was greater than 95% and the product was devoid of other chemical impurities including residual aluminum and acetonitrile. The biodistribution study in fibrosarcoma tumor model showed maximum uptake in tumor, 2 h post injection. Finally, PET/CT imaging studies in normal healthy rabbit, showed clear uptake in the organs involved in the metabolic process of MISO. No bone uptake was observed excluding the presence of free [18F]fluoride. The reported method can be easily adapted in any commercial FDG synthesis module. |
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