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Polymers 2017, 9(8), 362; https://doi.org/10.3390/polym9080362

Aromatic Modification of Low Molecular Weight PEI for Enhanced Gene Delivery

Key Laboratory of Green Chemistry and Technology (Ministry of Education), College of Chemistry, Sichuan University, Chengdu 610064, China
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Received: 17 July 2017 / Revised: 3 August 2017 / Accepted: 3 August 2017 / Published: 15 August 2017
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Abstract

Low molecular weight polyethylenimine (1800 Da, also referred to as oligoethylenimines, OEI) was modified with amino acids, including two aromatic amino acids (tryptophan, phenylalanine) and an aliphatic amino acid (leucine). The substitution degree of amino acids could be controlled by adjusting the feeding mole ratio of the reactants. Fluorescence spectroscopy and circular dichroism experiments demonstrated that the indole ring of tryptophan may intercalate into the DNA base pairs and contribute to efficient DNA condensation. In vitro gene expression results revealed that the modified OEIs (OEI-AAs) may provide higher transfection efficiency even than high molecular weight polyethylenimine (25 kDa, PEI), especially the aromatic tryptophan substituted OEI. Moreover, OEI-AAs exhibited excellent serum tolerance, and up to 137 times higher transfection efficiency than PEI 25 kDa that was obtained in the presence of serum. The cytotoxicity of OEI-AAs is much lower than PEI 25 kDa. This study may afford a new method for the development of low molecular weight oligomeric non-viral gene vectors with both high efficiency and biocompatibility. View Full-Text
Keywords: gene delivery; non-viral gene vector; LMW PEI; aromatic amino acid; structure-activity relationship gene delivery; non-viral gene vector; LMW PEI; aromatic amino acid; structure-activity relationship
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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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Yu, Q.-Y.; Zhan, Y.-R.; Zhang, J.; Luan, C.-R.; Wang, B.; Yu, X.-Q. Aromatic Modification of Low Molecular Weight PEI for Enhanced Gene Delivery. Polymers 2017, 9, 362.

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