| Literature DB >> 25176577 |
Harald R Krüger1, Irene Schütz2, Aileen Justies1, Kai Licha3, Pia Welker3, Volker Haucke2, Marcelo Calderón4.
Abstract
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.Entities:
Keywords: Drug delivery; FRET imaging; Intracellular release; Polymer therapeutic
Mesh:
Substances:
Year: 2014 PMID: 25176577 DOI: 10.1016/j.jconrel.2014.08.018
Source DB: PubMed Journal: J Control Release ISSN: 0168-3659 Impact factor: 9.776