Untiring Pursuit for Glucarate-Based Molecular Imaging Probes

Zhang, Dongjian; Jin, Qiaomei; Gao, Meng; Jiang, Cuihua; Ni, Yicheng; Zhang, Jian

doi:10.1007/s11307-020-01564-y

Cited by 2 publications

(1 citation statement)

References 51 publications

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“…However, due to the disparity between the volume of radioisotope solutions (~ 1 mL) and reaction volumes of microscale systems (as low as 1–10 s of µL), relatively small amounts of product activity have been acquired, suitable only for preclinical imaging 19 , 24 , 25 . Nevertheless, clinically-relevant quantities of various diagnostic radiopharmaceuticals has been produced with such microscale systems: [ 13 N]NH 3 26 , [ 68 Ga]Ga-PSMA-11 27 , [ 89 Zr]Zr-DFO-Trastuzamab 28 , [ 18 F]FDG 29 , 30 , [ 18 F]FET 31 , [ 18 F]fallypride 32 , 33 , [ 18 F]FT807 34 , [ 18 F]FPEB 35 , [ 18 F]FLT 36 and [ 18 F]FMISO 36 , 37 . A summary of reports of the 18 F-labeled ones is included in Table 1 .…”

Section: Introductionmentioning

confidence: 99%

Economical droplet-based microfluidic production of [18F]FET and [18F]Florbetaben suitable for human use

Lisova

Wang

Hajagos

et al. 2021

Sci Rep

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Current equipment and methods for preparation of radiopharmaceuticals for positron emission tomography (PET) are expensive and best suited for large-scale multi-doses batches. Microfluidic radiosynthesizers have been shown to provide an economic approach to synthesize these compounds in smaller quantities, but can also be scaled to clinically-relevant levels. Batch microfluidic approaches, in particular, offer significant reduction in system size and reagent consumption. Here we show a simple and rapid technique to concentrate the radioisotope, prior to synthesis in a droplet-based radiosynthesizer, enabling production of clinically-relevant batches of [18F]FET and [18F]FBB. The synthesis was carried out with an automated synthesizer platform based on a disposable Teflon-silicon surface-tension trap chip. Up to 0.1 mL (4 GBq) of radioactivity was used per synthesis by drying cyclotron-produced aqueous [18F]fluoride in small increments directly inside the reaction site. Precursor solution (10 µL) was added to the dried [18F]fluoride, the reaction chip was heated for 5 min to perform radiofluorination, and then a deprotection step was performed with addition of acid solution and heating. The product was recovered in 80 µL volume and transferred to analytical HPLC for purification. Purified product was formulated via evaporation and resuspension or a micro-SPE formulation system. Quality control testing was performed on 3 sequential batches of each tracer. The method afforded production of up to 0.8 GBq of [18F]FET and [18F]FBB. Each production was completed within an hour. All batches passed quality control testing, confirming suitability for human use. In summary, we present a simple and efficient synthesis of clinically-relevant batches of [18F]FET and [18F]FBB using a microfluidic radiosynthesizer. This work demonstrates that the droplet-based micro-radiosynthesizer has a potential for batch-on-demand synthesis of 18F-labeled radiopharmaceuticals for human use.

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