Microfluidic technology for PET radiochemistry

Microfluidic radiolabeling of biomolecules with PET radiometals

“…Effect of (a) residence time, and (b) temperature on the labeling of DOTA/NOTAcyclo(RGDfK) with carrier-added 64 Cu 2+ / 68 Ga 3+ . Comparison of radiolabeling results between two approaches, microreactor and conventional method: (a) labeling DOTA-RGD with carrier-added 68 Ga 3+ at different temperature (23,37 and 47 °C) with a residence time of 10 minutes; (b) labeling NOTA/DOTA-RGD with carrier-added 64 Cu 2+ / 68 Ga 3+ with a residence time of 10 minutes at 37 °C. Preparation of no-carrier added 64 Cu 2+ / 68 Ga 3+ labeled BFC-BM with different L: M ratio at 37 °C, and a residence time of 10 minutes for DOTA/NOTA-RGD peptides and a residence time of 20 minutes for DOTA-BSA proteins.…”

Application of tomography in microreactors

“…These reactions involved direct radioiodination of apoptosis marker annexin V using 124 I, the indirect radioiodination of the anticancer drug doxorubicin from a tinbutyl precursor, and the radiosynthesis of [ 18 F]FDG from a mannose triflate precursor and 18 F. They demonstrated the rapid radioiodination of the protein annexin V (40% RCY within 1 min) and the rapid radiofluorination of [ 18 F]FDG (60% RCY within 4 s) using a polymer microreactor chip. In addition, Gillies, Prenant, Chimon, Smethurst, Perrie, Dekker, et al (2006) and Gillies, Prenant, Chimon, Smethurst, Perrie, Hamblett, et al (2006) reported on a three-layer polycarbonate microreactor for radiolabeling the PET isotopes 18 F and 124 I, and SPECT (single-photon emission CT) isotope 99m Tc. In their study, the top plate of their device contains three inlets for reagents; the middle plate is a disc-shaped cavity with a simple vortex mixer, which also acts as an outlet to the bottom disc cavity containing an outlet port.…”

“…In the case of radiohalogenation of small-and large-molecular-weight molecules with a microfluidic device, Gillies, Prenant, Chimon, Smethurst, Perrie, Dekker, et al (2006) and Gillies, Prenant, Chimon, Smethurst, Perrie, Hamblett, et al (2006) used two microreactor devices in series to achieve two steps ([ 18 F] fluorination þ deprotection) required for [ 18 F]FDG synthesis. These reactions involved direct radioiodination of apoptosis marker annexin V using 124 I, the indirect radioiodination of the anticancer drug doxorubicin from a tinbutyl precursor, and the radiosynthesis of [ 18 F]FDG from a mannose triflate precursor and 18 F. They demonstrated the rapid radioiodination of the protein annexin V (40% RCY within 1 min) and the rapid radiofluorination of [ 18 F]FDG (60% RCY within 4 s) using a polymer microreactor chip.…”

Multiparametric Labeling Optimization and Synthesis of 68Ga-Labeled Compounds Applying a Continuous-Flow Microfluidic Methodology

“…Currently there are two major trends in the evolution of microfluidics, defined as continuous-and stop-flow setups [14,15]. The use of microreactors may be used to resolve some of currently existing limitations to biomolecule radiolabeling protocols [1,[16][17][18]. These constrains include features such as the ability to manipulate small volumes, ensure effective mixing and heat transfer, and the reduction of the system footprint.…”