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Correlation between Protonation of Tailor-Made Polypiperazines and Endosomal Escape for Cytosolic Protein Delivery

Title data

Hausig, Franziska ; Sobotta, Fabian H. ; Richter, Friederike ; Harz, Dominic O. ; Traeger, Anja ; Brendel, Johannes C.:
Correlation between Protonation of Tailor-Made Polypiperazines and Endosomal Escape for Cytosolic Protein Delivery.
In: ACS Applied Materials & Interfaces. Vol. 13 (2021) Issue 30 . - pp. 35233-35247.
ISSN 1944-8252
DOI: https://doi.org/10.1021/acsami.1c00829

Abstract in another language

Responsive polymers, which become protonated at decreasing pH, are considered a milestone in the development of synthetic cell entry vectors. Exact correlations between their properties and their ability to escape the endosome, however, often remain elusive due to hydrophobic interactions or limitations in the design of water-soluble materials with suitable basicity. Here, we present a series of well-defined, hydrophilic polypiperazines, where systematic variation of the amino moiety facilitates an unprecedented fine-tuning of the basicity or pKa value within the physiologically relevant range (pH 6–7.4). Coincubation of HEK 293T cells with various probes, including small fluorophores or functioning proteins, revealed a rapid increase of endosomal release for polymers with pKa values above 6.5 or 7 in serum-free or serum-containing media, respectively. Similarly, cytotoxic effects became severe at increased pKa values (>7). Although the window for effective transport appears narrow, the discovered correlations offer a principal guideline for the design of effective polymers for endosomal escape.

Further data

Item Type: Article in a journal
Refereed: Yes
Keywords: membrane leakage; calcein release; endosomolytic polymers; pH-responsive polymers; basicity
Institutions of the University: Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Chemistry > Chair Macromolecular Chemistry I
Faculties
Faculties > Faculty of Biology, Chemistry and Earth Sciences
Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Chemistry
Faculties > Faculty of Biology, Chemistry and Earth Sciences > Department of Chemistry > Chair Macromolecular Chemistry I > Chair Macromolecular Chemistry I - Univ.-Prof. Dr. Johannes C. Brendel
Result of work at the UBT: No
DDC Subjects: 500 Science > 540 Chemistry
Date Deposited: 21 Feb 2024 07:25
Last Modified: 02 May 2024 07:39
URI: https://eref.uni-bayreuth.de/id/eprint/88588