A cationic poly(2-oxazoline) with high in vitro transfection efficiency identified by a library approach.
A cationic poly(2-oxazoline) with high in vitro transfection efficiency identified by a library approach.
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DOI：
10.1002/mabi.201400334
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发表时间：
2015-03
影响因子：
4.6
通讯作者：
Alexandra C. Rinkenauer;L. Tauhardt;F. Wendler;K. Kempe;M. Gottschaldt;Anja Traeger;U. Schubert
中科院分区：
文献类型：
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作者：
Alexandra C. Rinkenauer;L. Tauhardt;F. Wendler;K. Kempe;M. Gottschaldt;Anja Traeger;U. Schubert
迄今为止，具有高转染效率（TE）的阳离子聚合物通常具有高细胞毒性。通过筛选基于阳离子2-恶唑啉的18元聚合物文库，可以鉴定出具有与线性聚（乙烯亚胺）相似的TE但在所研究浓度下没有检测到细胞毒性的聚合物。研究了聚合物侧链疏水性、氨基类型和含量对pDNA缩聚、TE、细胞毒性、细胞膜相互作用以及多聚物的大小、电荷和稳定性的影响。高效TE需要伯胺和至少40%的胺含量。而具有短侧链的聚合物在胺含量达40%时无毒，而长疏水侧链则引起高细胞毒性。
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.