Details

Autor(en) / Beteiligte

• Krüger, Harald R.
• Schütz, Irene
• Justies, Aileen
• Licha, Kai
• Welker, Pia
• Haucke, Volker
• Calderón, Marcelo

Titel

Imaging of doxorubicin release from theranostic macromolecular prodrugs via fluorescence resonance energy transfer

Ist Teil von

• Journal of controlled release, 2014-11, Vol.194, p.189-196

Ort / Verlag

Netherlands: Elsevier B.V

Erscheinungsjahr

2014

Quelle

MEDLINE

Beschreibungen/Notizen

• Herein we present a FRET-based theranostic macromolecular prodrug (TMP) composed of (a) dendritic polyglycerol (PG) as polymeric nanocarrier, (b) doxorubicin (Dox) linked via a pH-sensitive hydrazone to (c) a tri-functional linker, and (d) an indodicarbocyanine dye (IDCC) attached in close proximity to Dox. The drug fluorescence is quenched via intramolecular FRET until the pH-sensitive hydrazone bond between the TMP and Dox is cleaved at acidic pH. By measuring its fluorescence, we characterized the TMP cleavage kinetics at different pH values in vitro. The intracellular release of Dox from the carrier was monitored in real time in intact cancer cells, giving more insight into the mode of action of a polymer drug conjugate. Caught in action. A theranostic macromolecular prodrug that allows monitoring the intracellular doxorubicin release in real time has been designed. [Display omitted]