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Open AccessArticle

Comparative Study of Diethylaminoethyl-Chitosan and Methylglycol-Chitosan as Potential Non-Viral Vectors for Gene Therapy

Institute of Macromolecular Compounds of the Russian Academy of Sciences, Bolshoi pr. VO 31, St. Petersburg 199004, Russia
Institute of Chemistry, St. Petersburg State University, Universitetskii pr. 26, Petrodvorets, St. Petersburg 198504, Russia
University of Vienna, Althanstrasse, 14, A-1090 Vienna, Austria
Department of Biomolecular Sciences, School of Pharmacy, University of Urbino, 61029 Urbino, Italy
Department of Pharmacology & Pharmacy, Li Ka Shing Faculty of Medicine, The University of Hong Kong, 21 Sassoon Road, Pokfulam, Hong Kong, China
Department of Chemical Sciences, University of Huddersfield, Huddersfield HD1 3DH, UK
Research Institute of Influenza, ul. Prof. Popova 15/17, St. Petersburg 197376, Russia
Peter the Great St. Petersburg Polytechnic University, Polytechnicheskaya ul. 29, St. Petersburg 195251, Russia
Institute of Experimental Medicine, Almazov National Medical Research Centre, ul. Akkuratova 2, St. Petersburg 197341, Russia
Author to whom correspondence should be addressed.
Polymers 2018, 10(4), 442;
Received: 5 March 2018 / Revised: 11 April 2018 / Accepted: 11 April 2018 / Published: 14 April 2018
(This article belongs to the Collection Polysaccharides)
In this paper, we compared the transfection efficiency and cytotoxicity of methylglycol-chitosan (MG-CS) and diethylaminoethyl-chitosan (DEAE-CSI and DEAE-CSII with degrees of substitution of 1.2 and 0.57, respectively) to that of Lipofectamine (used as a reference transfection vector). MG-CS contains quaternary amines to improve DNA binding, whereas the DEAE-CS exhibits pH buffering capability that would ostensibly enhance transfection efficiency by promoting endosomal escape. Gel retardation assays showed that both DEAE-CS and MG-CS bound to DNA at a polysaccharide:DNA mass ratio of 2:1. In Calu-3 cells, the DNA transfection activity was significantly better with MG-CS than with DEAE-CS, and the efficiency improved with increasing polysaccharide:DNA ratios. By contrast, the efficiency of DEAE-CSI and DEAE-CSII was independent of the polysaccharide:DNA ratio. Conversely, in the transfection-recalcitrant JAWSII cells, both Lipofectamine and MG-CS showed significantly lower DNA transfection activity than in Calu-3 cells, whereas the efficiency of DEAE-CSI and DEAE-CSII was similar in both cell lines. The toxicity of DEAE-CS increased with increasing concentrations of the polymer and its degree of substitution, whereas MG-CS demonstrated negligible cytotoxicity, even at the highest concentration studied. Overall, MG-CS proved to be a more efficient and less toxic transfection agent when compared to DEAE-CS. View Full-Text
Keywords: diethylaminoethyl-chitosan; methylglycol-chitosan; polyplex; cell transfection; gene delivery diethylaminoethyl-chitosan; methylglycol-chitosan; polyplex; cell transfection; gene delivery
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MDPI and ACS Style

Raik, S.V.; Andranovitš, S.; Petrova, V.A.; Xu, Y.; Lam, J.K.-W.; Morris, G.A.; Brodskaia, A.V.; Casettari, L.; Kritchenkov, A.S.; Skorik, Y.A. Comparative Study of Diethylaminoethyl-Chitosan and Methylglycol-Chitosan as Potential Non-Viral Vectors for Gene Therapy. Polymers 2018, 10, 442.

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