Copper-catalyzed click reactions: quantification of retained copper using 64Cu-spiked Cu(I), exemplified for CuAAC reactions on liposomes
- Publication type:
- Journal article
- Metadata:
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- Abstract
- <jats:title>Abstract</jats:title> <jats:p>The Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC) is a powerful, highly reliable and selective reaction which allows for a rapid synthesis in high yields and under mild conditions (pH, temperature). However, the cytotoxicity of copper requires its complete removal prior to an application <jats:italic>in vivo</jats:italic>. This is an issue especially when it comes to CuAAC reactions on macromolecular structures or drug delivery systems, as copper might be retained by these systems. Thus, a quantification of the final copper content of these systems is inevitable, which we exemplified for a CuAAC reaction on liposomes using <jats:sup>64</jats:sup>Cu-spiked Cu(I). In this respect, a Cu(II) nitrate solution was irradiated at the TRIGA Mark II research reactor Mainz to obtain <jats:italic>c.a.</jats:italic> [<jats:sup>64</jats:sup>Cu]Cu(II). The irradiated solution was directly used for a CuAAC on liposomes. After purification, their copper content was calculated utilizing γ-ray spectrometry. Only 0.018% of the added <jats:sup>64</jats:sup>Cu-activity was still present in the liposome containing fractions after purification. This refers to a total amount of copper of 0.17 ng. The amount of retained copper is so low, that an <jats:italic>in vivo</jats:italic> application of the liposomes is absolutely reasonable. Besides this particular study, the experimental methodology may be applied to study many other CuAAC reactions, used for the synthesis of radiolabeled or non-radioactive species, which are intended for human applications.</jats:p>
- Autoren
- Karolin Wagener
- Dennis Renisch
- Meike Schinnerer
- Matthias Worm
- Yvonne Jakob
- Klaus Eberhardt
- Frank Rösch
- DOI
- 10.1515/ract-2018-3000
- eISSN
- 2193-3405
- ISSN
- 0033-8230
- Ausgabe der Veröffentlichung
- 7
- Zeitschrift
- Radiochimica Acta
- Sprache
- en
- Online publication date
- 2018
- Paginierung
- 547 - 554
- Datum der Veröffentlichung
- 2019
- Status
- Published
- Herausgeber
- Walter de Gruyter GmbH
- Herausgeber URL
- http://dx.doi.org/10.1515/ract-2018-3000
- Datum der Datenerfassung
- 2023
- Titel
- Copper-catalyzed click reactions: quantification of retained copper using <sup>64</sup>Cu-spiked Cu(I), exemplified for CuAAC reactions on liposomes
- Ausgabe der Zeitschrift
- 107
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