title: Microfluidic technology for PET radiochemistry.
abstract: This paper describes the first application of a microfabricated reaction system to positron emission tomography (PET) radiochemistry. We have applied microfluidic technology to synthesise PET radiopharmaceuticals using (18)F and (124)I as labels for fluorodeoxyglucose (FDG) and Annexin-V, respectively. These reactions involved established methods of nucleophilic substitution on a mannose triflate precursor and direct iodination of the protein using iodogen as an oxidant. This has demonstrated a proof of principle of using microfluidic technology to radiochemical reactions involving low and high molecular weight compounds. Using microfluidic reactions, [(18)F]FDG was synthesised with a 50% incorporation of the available F-18 radioactivity in a very short time of 4s. The radiolabelling efficiency of (124)I Annexin-V was 40% after 1 min reaction time. Chromatographic analysis showed that such reaction yields are comparable to conventional methods, but in a much shorter time. The yields can be further improved with more optimisation of the microfluidic device itself and its fluid mixing profiles. This demonstrates the potential for this technology to have an impact on rapid and simpler radiopharmaceutical synthesis using short and medium half-life radionuclides.
authors.affiliation: Cancer Research-UK/University of Manchester Radiochemical Targeting and Imaging Group, Paterson Institute for Cancer Research, Manchester M20 4BX, UK. jgillies@picr.man.ac.uk
authors.forename: J M
authors.initials: JM
authors.lastname: Gillies
authors.forename: C
authors.initials: C
authors.lastname: Prenant
authors.forename: G N
authors.initials: GN
authors.lastname: Chimon
authors.forename: G J
authors.initials: GJ
authors.lastname: Smethurst
authors.forename: B A
authors.initials: BA
authors.lastname: Dekker
authors.forename: J
authors.initials: J
authors.lastname: Zweit
mesh_terms: D001709:Biotechnology / Q000295:instrumentation* / Q000379:methods; D004867:Equipment Design; D019544:Equipment Failure Analysis; D005240:Feasibility Studies; D019788:Fluorodeoxyglucose F18 / Q000737:chemistry* / Q000302:isolation & purification; D007553:Isotope Labeling / Q000295:instrumentation* / Q000379:methods; D046210:Microfluidic Analytical Techniques / Q000295:instrumentation* / Q000379:methods; D049268:Positron-Emission Tomography / Q000295:instrumentation* / Q000379:methods; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000302:isolation & purification
chemical_list: D019275:Radiopharmaceuticals; D019788:Fluorodeoxyglucose F18