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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

Chittimalla Chandrashekhar, Bénédicte Pons, Christian D Muller, Nassera Tounsi, Rita Mulherkar, Guy Zuber

Acta Biomater. 2013 Feb;9(2):4985-93.

PMID: 23000009

Abstract:

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP9002986	Polyethylenimine, linear		9002-98-6	Price

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