Oligobenzylethylenimine enriches linear polyethylenimine with a pH-sensitive membrane-disruptive property and leads to enhanced gene delivery activity
Oligobenzylethylenimine enriches linear polyethylenimine with a pH-sensitive membrane-disruptive property and leads to enhanced gene delivery activity
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DOI：
10.1016/j.actbio.2012.09.015
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发表时间：
2013-02-01
影响因子：
9.7
通讯作者：
Zuber, Guy
中科院分区：
文献类型：
--
作者：
Chandrashekhar, Chittimalla;Pons, Benedicte;Zuber, Guy
本文报道了一种二嵌段线性聚合物寡（苄基乙烯亚胺）-b-聚乙烯亚胺（OBzEI-PEI）的合成，并研究了其基因传递特性。线性共聚物OBzEI-PEI是通过二嵌段聚恶唑啉的酸水解以简单的方式制备的，该二嵌段聚恶唑啉是通过4-苄基-2-乙基-2-恶唑啉然后2-乙基-2-恶唑啉的顺序聚合制成的。新聚合物的pH滴定和DNA络合概况与常规线性PEI相似，但在各种细胞系中具有更高的基因转染效率，尽管细胞对质粒DNA的摄取减少。进一步的实验表明，OBzEI尾补充了PEI的固有质子海绵内体溶解活性与酸pH敏感性膜扰动活性。(C)2012 Acta Materialia Inc.由爱思唯尔有限公司出版。保留所有权利。
We report here the synthesis of a diblock linear polymer of oligo(benzylethylenimine)-b-polyethylenimine (OBzEI-PEI) and investigate its gene delivery properties. The linear copolymer OBzEI-PEI was prepared in a straightforward manner by acidic hydrolysis of a diblock polyoxazoline, which had been made by sequential polymerization of 4-benzyl-2-ethyl-2-oxazoline followed by 2-ethyl-2-oxazoline. pH titration and DNA complexation profiles of the new polymer are similar to regular linear PEIs, but with higher gene transfection efficiencies in various cell lines despite a decreased cellular uptake of plasmid DNA. Further experiments suggest that the OBzEI tail complements the intrinsic proton-sponge endosomolytic activities of PEI with an acid pH-sensitive membrane-perturbing activity. (C) 2012 Acta Materialia Inc. Published by Elsevier Ltd. All rights reserved.