Radiolabeling of DOTA-like conjugated peptides with generator-produced Ga-68 and using NaCl-based cationic elution method
| Autor: | Andreas Odparlik, Ingo Klette, Dirk Mueller, Michael K. Schultz, Wouter A.P. Breeman, Michael Gottschaldt, Manfred Baehre, Izabela Tworowska |
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| Přispěvatelé: | Radiology & Nuclear Medicine |
| Rok vydání: | 2016 |
| Předmět: |
chemistry.chemical_classification
Chromatography Ion exchange Elution Sodium Cationic polymerization chemistry.chemical_element Gallium Radioisotopes Peptide Hydrochloric acid Sodium Chloride High-performance liquid chromatography Article General Biochemistry Genetics and Molecular Biology 030218 nuclear medicine & medical imaging Heterocyclic Compounds 1-Ring 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine chemistry Isotope Labeling 030220 oncology & carcinogenesis DOTA Peptides |
| Zdroj: | Nature protocols Nature Protocols, 11(6), 1057-1066. Nature Publishing Group |
| ISSN: | 1754-2189 |
| DOI: | 10.1038/nprot.2016.060 |
| Popis: | Gallium-68 ((68)Ga) is a generator-produced radionuclide with a short half-life (t½ = 68 min) that is particularly well suited for molecular imaging by positron emission tomography (PET). Methods have been developed to synthesize (68)Ga-labeled imaging agents possessing certain drawbacks, such as longer synthesis time because of a required final purification step, the use of organic solvents or concentrated hydrochloric acid (HCl). In our manuscript, we provide a detailed protocol for the use of an advantageous sodium chloride (NaCl)-based method for radiolabeling of chelator-modified peptides for molecular imaging. By working in a lead-shielded hot-cell system,(68)Ga(3+) of the generator eluate is trapped on a cation exchanger cartridge (100 mg, ∼8 mm long and 5 mm diameter) and then eluted with acidified 5 M NaCl solution directly into a sodium acetate-buffered solution containing a DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) or DOTA-like chelator-modified peptide. The main advantages of this procedure are the high efficiency and the absence of organic solvents. It can be applied to a variety of peptides, which are stable in 1 M NaCl solution at a pH value of 3-4 during reaction. After labeling, neutralization, sterile filtration and quality control (instant thin-layer chromatography (iTLC), HPLC and pH), the radiopharmaceutical can be directly administered to patients, without determination of organic solvents, which reduces the overall synthesis-to-release time. This procedure has been adapted easily to automated synthesis modules, which leads to a rapid preparation of (68)Ga radiopharmaceuticals (12-16 min). |
| Databáze: | OpenAIRE |
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