Earley, D.F.; Guillou, A.; van der Born, D.; Poot, A.J.; Holland, J.P. Microfluidic Preparation of 89Zr-Radiolabelled Proteins by Flow Photochemistry. Molecules2021, 26, 764.
Earley, D.F.; Guillou, A.; van der Born, D.; Poot, A.J.; Holland, J.P. Microfluidic Preparation of 89Zr-Radiolabelled Proteins by Flow Photochemistry. Molecules 2021, 26, 764.
Abstract
89Zr-radiolabelled proteins functionalised with desferrioxamine B are a cornerstone of diagnostic positron emission tomography. In the clinical setting, 89Zr-labelled proteins are produced manually. Here, we explore the potential of using a microfluidic photochemical flow reactor to prepare 89Zr-radiolabelled proteins. The light-induced functionalisation and 89Zr-radiolabelling of human serum albumin ([89Zr]ZrDFO-PEG3-Et-azepin-HSA) was achieved by flow photochemistry with a decay-corrected radiochemical yield (RCY) of 31.2±1.3% (n = 3) and radiochemical purity >90%. In comparison, a manual batch photoreactor synthesis produced the same radiotracer in a decay-corrected RCY of 59.6±3.6% (n = 3) with an equivalent RCP >90%. The results indicate that photoradiolabelling in flow is a feasible platform for the automated production of protein-based 89Zr-radiotracers, but further refinement of the apparatus, and optimisation of the method is required before the flow process is competitive with manual reactions.
Subject Areas
Flow Chemistry; Photochemistry; Radiochemistry; Protein Conjugation.
Copyright:
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Daniel F. Earley