Scalable droplet-based radiosynthesis of [18F]fluorobenzyltriphenylphosphonium cation ([18F]FBnTP) via a “numbering up” approach

Lu, Yingqing; Collins, Jeffrey; Lin, Kuo-Shyan; van Dam, R. Michael

doi:10.1039/d3lc01068f

Lab Chip

2024

DOI: 10.1039/d3lc01068f

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Scalable droplet-based radiosynthesis of [¹⁸F]fluorobenzyltriphenylphosphonium cation ([¹⁸F]FBnTP) via a “numbering up” approach

Yingqing Lu,

Jeffrey Collins,

Kuo-Shyan Lin

et al.

Abstract: The [18F]fluorobenzyltriphenylphosphonium cation ([18F]FBnTP) has emerged as a highly promising positron emission tomography (PET) tracer for myocardial perfusion imaging (MPI) due to its uniform distribution in the myocardium and favorable...

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References 31 publications

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Rapid Concentration of Ga-68 and Proof-of-Concept Microscale Labeling of [68Ga]Ga-PSMA-11 in a Droplet Reactor

Lu,

Chao,

Collins

et al. 2024

Molecules

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The radiometal gallium-68 (Ga-68) has garnered significant interest due to its convenient production via compact and widely available generators and the high performance of 68Ga-labeled compounds for positron-emission tomography (PET) imaging for cancer diagnosis and management of patients undergoing targeted radionuclide therapy. Given the short half life of Ga-68 (68 min), microfluidic-based radiosynthesis is a promising avenue to establish very rapid, efficient, and routine radiolabeling with Ga-68; however, the typical elution volume of Ga-68 from a generator (4–10 mL) is incompatible with the microliter reaction volumes of microfluidic devices. To bridge this gap, we developed a microscale cartridge-based approach to concentrate Ga-68. By optimizing cartridge design, resin type, resin mass, and eluent composition, Ga-68 was reliably concentrated from ~6 mL to ~80 µL with high recovery efficiency (>97%, n = 14). Furthermore, this method is suitable for both single- and dual-generator setups. To demonstrate suitability of the concentrated radiometal for radiolabeling, we performed microdroplet synthesis of [68Ga]Ga-PSMA-11, achieving high radiochemical yield (83 ± 11%, n = 3), excellent radiochemical purity (>99%), and high apparent specific activity (255–320 MBq/μg). The entire process, including Ga-68 concentration, radiosynthesis, purification, and formulation, was completed in 12 min. Starting with activity of 0.81–0.84 GBq, 0.51–0.64 GBq of product was produced, sufficient for multiple patient doses. This work paves the way to clinical-scale production of other 68Ga-labeled compounds using droplet microreactor methods, or high-throughput labeling optimization or compound screening of 68Ga-labeled probes using droplet reaction arrays.

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Rapid Concentration of Ga-68 and Proof-of-Concept Microscale Labeling of [68Ga]Ga-PSMA-11 in a Droplet Reactor

Lu,

Chao,

Collins

et al. 2024

Molecules

View full text Add to dashboard Cite

show abstract

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Scalable droplet-based radiosynthesis of [¹⁸F]fluorobenzyltriphenylphosphonium cation ([¹⁸F]FBnTP) via a “numbering up” approach

Abstract: The [18F]fluorobenzyltriphenylphosphonium cation ([18F]FBnTP) has emerged as a highly promising positron emission tomography (PET) tracer for myocardial perfusion imaging (MPI) due to its uniform distribution in the myocardium and favorable...

Cited by 1 publication

References 31 publications

Rapid Concentration of Ga-68 and Proof-of-Concept Microscale Labeling of [68Ga]Ga-PSMA-11 in a Droplet Reactor

Rapid Concentration of Ga-68 and Proof-of-Concept Microscale Labeling of [68Ga]Ga-PSMA-11 in a Droplet Reactor

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