TY - JOUR
T1 - A cationic poly(2-oxazoline) with high in vitro transfection efficiency identified by a library approach
AU - Rinkenauer, Alexandra C.
AU - Tauhardt, Lutz
AU - Wendler, Felix
AU - Kempe, Kristian
AU - Gottschaldt, Michael
AU - Traeger, Anja
AU - Schubert, Ulrich S.
PY - 2015
Y1 - 2015
N2 - 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.
AB - 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.
KW - Gene delivery
KW - Hydrophobic side chain
KW - Poly(2-oxazoline)s
KW - Primary amine
KW - Structure-property relationship
KW - Tertiary amine
KW - Viability
UR - http://www.scopus.com/inward/record.url?scp=84924024760&partnerID=8YFLogxK
U2 - 10.1002/mabi.201400334
DO - 10.1002/mabi.201400334
M3 - Article
C2 - 25403084
AN - SCOPUS:84924024760
SN - 1616-5187
VL - 15
SP - 414
EP - 425
JO - Macromolecular Bioscience
JF - Macromolecular Bioscience
IS - 3
ER -