Microfluidic Preparation of 89Zr-Radiolabelled Proteins by Flow Photochemistry

Molecules

Amaury Guillou¹  DanielF. Earley¹  JasonP. Holland¹  AlexJ. Poot²  Dion van der Born³ 

[1] Department of Chemistry, University of Zurich, Winterthurerstrasse 190, CH-8057 Zurich, Switzerland;Department of Radiology and Nuclear Medicine, UMC Utrecht, Heidelberglaan 100, 3584 CX Utrecht, The Netherlands;FutureChemistry Agro Business Park 10, 6708 PW Wageningen, The Netherlands;

关键词: flow chemistry;    photochemistry;    radiochemistry;    protein conjugation;   

DOI  :  10.3390/molecules26030764

来源: DOAJ

【 摘 要 】

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 are required before the flow process is competitive with manual reactions.

【 授权许可】

Unknown