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Angew Chem Int Ed Engl. 2016 Nov 14;55(47):14842-14846. doi: 10.1002/anie.201606065. Epub 2016 Oct 24.

Nanoscale Biodegradable Organic-Inorganic Hybrids for Efficient Cell Penetration and Drug Delivery.

Author information

1
Clemens-Schöpf-Institut für Organische Chemie und Biochemie, Technische Universität Darmstadt, Alarich-Weiss-Strasse 4, 64287, Darmstadt, Germany.
2
Clemens-Schöpf-Institut für Organische Chemie und Biochemie, Technische Universität Darmstadt, Alarich-Weiss-Strasse 16, 64287, Darmstadt, Germany.
3
Institut für Organische und Biomolekulare Chemie, Georg-August Universität Göttingen, Tammannstrasse 2, 37077, Göttingen, Germany.

Abstract

We report a comprehensive study on novel, highly efficient, and biodegradable hybrid molecular transporters. To this end, we designed a series of cell-penetrating, cube-octameric silsesquioxanes (COSS), and investigated cellular uptake by confocal microscopy and flow cytometry. A COSS with dense spatial arrangement of guanidinium groups displayed fast uptake kinetics and cell permeation at nanomolar concentrations in living HeLa cells. Efficient uptake was also observed in bacteria, yeasts, and archaea. The COSS-based carrier was significantly more potent than cell-penetrating peptides (CPPs) and displayed low toxicity. It efficiently delivered a covalently attached cytotoxic drug, doxorubicin, to living tumor cells. As the uptake of fluorescently labeled carrier remained in the presence of serum, the system could be considered particularly attractive for the in vivo delivery of therapeutics.

KEYWORDS:

COSS; cell penetration; cell-penetrating compound; drug delivery; silsesquioxanes

PMID:
27774725
DOI:
10.1002/anie.201606065
[Indexed for MEDLINE]

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