Multiparametric labeling optimization and synthesis of 68Ga-labeled compounds applying a continuous-flow microfluidic methodology

Gábor Máté, Dezso Szikra, Jakub Šimeček, Szandra Szilágyi, György Trencsényi, Hans Jürgen Wester, István Kertész, László Galuska

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

The synthesis and functional evaluation of a wide variety of radiolabeled chelator-biomolecule conjugates with high specific activity and radiochemical purity are crucial to development of personalized nuclear medicine. An excellent platform technology for achieving this objective involves use of generator-produced positron emission tomography (PET)-radionuclide 68Ga. Currently, applied manual methodology for optimization and development for new labeling techniques offers only slow screening with relatively high precursor consumption. A capillary-based microfluidic synthesis module with online high-performance liquid chromatography (HPLC) was constructed for the optimization of reaction parameters of 68Ga-PET tracers. This approach enables performance of 68Ga-labeling reactions in 10 μL volumes, followed by sample analysis. The high-throughput capacity of the system allows very rapid optimization. The optimal pH and ligand concentration from the experiments were utilized directly to the production of 68Ga-NODAGA-(RGD)2 and 68Ga-NOPO-RGD. Applying optimal parameters to production of these aforementioned radiopharmaceuticals allowed their synthesis with high radiochemical purity (over 95%) and with surprisingly negligible retention of residual activity in the system.

Original languageEnglish
Pages (from-to)86-93
Number of pages8
JournalJournal of Flow Chemistry
Volume6
Issue number2
DOIs
Publication statusPublished - Jun 2016

Keywords

  • Chelators
  • Gallium
  • Microfluidics
  • Positron emission tomography
  • RGD conjugates

ASJC Scopus subject areas

  • Chemistry (miscellaneous)
  • Fluid Flow and Transfer Processes
  • Organic Chemistry

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