Optimization of Radiochemical Reactions using Droplet Arrays.
Optimization of Radiochemical Reactions using Droplet Arrays.
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DOI：
10.3791/62056
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发表时间：
2021-02-12
期刊：
影响因子：
--
通讯作者：
van Dam RM
中科院分区：
文献类型：
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作者：
Rios A;Holloway TS;Wang J;van Dam RM
目前的自动放射合成器被设计用于生产大量临床批次的放射性药物。它们不太适合于反应优化或新型放射性药物开发，因为每个数据点涉及显著的试剂消耗，并且设备的污染在下一次使用之前需要时间进行放射性衰变。为了解决这些限制，开发了一种用于并行执行基于微型液滴的反应的阵列的平台，每个反应被限制在图案化的聚乙烯涂覆的硅“芯片”上的表面张力阱内。这些芯片能够快速方便地研究反应参数，包括试剂浓度、反应溶剂、反应温度和时间。该平台允许在几天内完成数百个反应，而试剂消耗最少，而不是使用传统的放射性合成仪需要数月。该方法描述了一种新的高通量方法的使用，基于液滴化学反应，用于使用纳摩尔量的试剂快速和经济地优化放射性药物。
Current automated radiosynthesizers are designed to produce large clinical batches of radiopharmaceuticals. They are not well suited for reaction optimization or novel radiopharmaceutical development since each data point involves significant reagent consumption, and contamination of the apparatus requires time for radioactive decay before the next use. To address these limitations, a platform for performing arrays of miniature droplet-based reactions in parallel, each confined within a surface-tension trap on a patterned polytetrafluoroethylene-coated silicon “chip”, was developed. These chips enable rapid and convenient studies of reaction parameters including reagent concentrations, reaction solvent, reaction temperature and time. This platform permits the completion of hundreds of reactions in a few days with minimal reagent consumption, instead of taking months using a conventional radiosynthesizer. This method describes the use of a novel high-throughput methodology, based on droplet chemical reactions, for the rapid and economical optimization of radiopharmaceuticals using nanomole amounts of reagents.