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Issue 9, 2015
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Dendritic polymer imaging systems for the evaluation of conjugate uptake and cleavage

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Abstract

Fluorescent turn-on probes combined with polymers have a broad range of applications, e.g. for intracellular sensing of ions, small molecules, or DNA. In the field of polymer therapeutics, these probes can be applied to extend the in vitro characterization of novel conjugates beyond cytotoxicity and cellular uptake studies. This is particularly true in cases in which polymer conjugates contain drugs attached by cleavable linkers. Better information on the intracellular linker cleavage and drug release would allow a faster evaluation and optimization of novel polymer therapeutic concepts. We therefore developed a fluorescent turn-on probe that enables direct monitoring of pH-mediated cleavage processes over time. This is achieved by exploiting the fluorescence resonance energy transfer (FRET) between two dyes that have been coupled to a dendritic polymer. We demonstrate the use of this probe to evaluate polymer uptake and intracellular release of cargo in a cell based microplate assay that is suitable for high throughput screening.

Graphical abstract: Dendritic polymer imaging systems for the evaluation of conjugate uptake and cleavage

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Publication details

The article was received on 04 Aug 2014, accepted on 26 Oct 2014 and first published on 03 Nov 2014


Article type: Paper
DOI: 10.1039/C4NR04467C
Citation: Nanoscale, 2015,7, 3838-3844
  • Open access: Creative Commons BY-NC license
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    Dendritic polymer imaging systems for the evaluation of conjugate uptake and cleavage

    H. R. Krüger, G. Nagel, S. Wedepohl and M. Calderón, Nanoscale, 2015, 7, 3838
    DOI: 10.1039/C4NR04467C

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