A cationic poly(2-oxazoline) with high in vitro transfection efficiency identified by a library approach

Alexandra C. Rinkenauer, Lutz Tauhardt, Felix Wendler, Kristian Kempe, Michael Gottschaldt, Anja Traeger, Ulrich S. Schubert

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27 Citations (Scopus)

Abstract

To date, cationic polymers with high transfection efficiencies (TE) often have a high cytotoxicity. By screening an 18-membered library of cationic 2-oxazoline-based polymers, a polymer with similar TE as linear poly(ethylene imine) but no detectable cytotoxicity at the investigated concentrations could be identified. The influence of the polymer side chain hydrophobicity and the type and content of amino groups on the pDNA condensation, the TE, the cytotoxicity, the cellular membrane interaction as well as the size, charge, and stability of the polyplexes was studied. Primary amines and an amine content of at least 40% were required for an efficient TE. While polymers with short side chains were non-toxic up to an amine content of 40%, long hydrophobic side chains induced a high cytotoxicity.

Original languageEnglish
Pages (from-to)414-425
Number of pages12
JournalMacromolecular Bioscience
Volume15
Issue number3
DOIs
Publication statusPublished - 2015
Externally publishedYes

Keywords

  • Gene delivery
  • Hydrophobic side chain
  • Poly(2-oxazoline)s
  • Primary amine
  • Structure-property relationship
  • Tertiary amine
  • Viability

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