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Polymers 2015, 7(11), 2316-2331;

Amino Acid-Modified Polyethylenimines with Enhanced Gene Delivery Efficiency and Biocompatibility

Key Laboratory of Green Chemistry and Technology (Ministry of Education), College of Chemistry, Sichuan University, Chengdu 610064, China
National Key Laboratory of Shock Wave and Detonation Physics, Institute of Fluid Physics, Chinese Academy of Engineering Physics, Mianyang 621900, China
West China School of Medicine, Sichuan University, Chengdu 610041, China
Humanwell Healthcare (Group) Co., LTD., 666 Gaoxin Road, East Lake High-Tech Development Zone, Wuhan 430075, China
Authors to whom correspondence should be addressed.
Academic Editor: Jianxun Ding
Received: 25 August 2015 / Revised: 2 November 2015 / Accepted: 10 November 2015 / Published: 17 November 2015
(This article belongs to the Special Issue Functional Polymers for Medical Applications)
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The development of gene delivery vectors with high efficiency and biocompatibility is one of the key points of gene therapy. A series of polycations were prepared from polyethylenimine (PEI) with several amino acids or their analogs. The target polymers have different charge and hydrophilic/hydrophobic properties, which may affect their performance in the gene transfection process. Gel retardation and DLS assays showed that these polymers may condense DNA into nanoparticles with positive zeta potentials and proper sizes for cellular uptake. Luciferase reporter gene transfection results revealed their higher transfection efficiency than PEI; especially in the presence of serum, in which up to 23 times higher efficiency was achieved by employing glycolic acid-grafted PEI. Moreover, it was found that the degree of substitution on PEI has an apparent influence on the transfection, and the balance between electron-positive/negative groups largely affects the delivery process. The higher serum tolerance was also proven by BSA adsorption, flow cytometry and confocal microscopy assays. Results demonstrate that such type of polycations may serve as promising non-viral gene delivery vectors. View Full-Text
Keywords: gene delivery; polyethylenimine; non-viral gene vector; biocompatibility gene delivery; polyethylenimine; non-viral gene vector; biocompatibility

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Zhang, Q.-F.; Luan, C.-R.; Yin, D.-X.; Zhang, J.; Liu, Y.-H.; Peng, Q.; Xu, Y.; Yu, X.-Q. Amino Acid-Modified Polyethylenimines with Enhanced Gene Delivery Efficiency and Biocompatibility. Polymers 2015, 7, 2316-2331.

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