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Guanidinylation: A simple way to fabricate cell penetrating peptide analogue-modified chitosan vector for enhanced gene delivery

Authors

  • Xinyun Zhai,

    1. School of Materials Science and Engineering, Tianjin Key Laboratory of Composite and Functional Materials, Tianjin University, Tianjin 300072, China
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  • Peng Sun,

    1. School of Materials Science and Engineering, Tianjin Key Laboratory of Composite and Functional Materials, Tianjin University, Tianjin 300072, China
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  • Yongfeng Luo,

    1. State Key Laboratory of Respiratory Disease and Guangzhou Institute of Respiratory Disease, Guangzhou Medical College, Guangzhou 510120, Guangdong Province, China
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  • Chaonan Ma,

    1. State Key Laboratory of Respiratory Disease and Guangzhou Institute of Respiratory Disease, Guangzhou Medical College, Guangzhou 510120, Guangdong Province, China
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  • Jun Xu,

    1. State Key Laboratory of Respiratory Disease and Guangzhou Institute of Respiratory Disease, Guangzhou Medical College, Guangzhou 510120, Guangdong Province, China
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  • Wenguang Liu

    Corresponding author
    1. School of Materials Science and Engineering, Tianjin Key Laboratory of Composite and Functional Materials, Tianjin University, Tianjin 300072, China
    • School of Materials Science and Engineering, Tianjin Key Laboratory of Composite and Functional Materials, Tianjin University, Tianjin 300072, China===

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Abstract

In view of the analogous transmembrane function to cell penetrating peptides, guanidine group was incorporated into chitosan by chemical modification to enhance the transfection performance of chitosan vectors. Guanidinylated chitosan (GCS) was shown to be well soluble in neutral aqueous solution. The interaction between GCS with plasmid DNA was characterized by agarose retardation experiment and ethidium bromide displacement assay. GCS formed more stable complexes with DNA under physiological pH than chitosan. The transfection efficiency of GCS was evaluated employing COS-7 cell line—GCS polyplexes demonstrated higher transfection efficiency and lower cytotoxicity relative to chitosan. The optimum efficiency of GCS was achieved in the vicinity of the critical complexing ratio. The results of flow cytometry indicated that guanidinylation promoted an eightfold increase in the cell uptake. The study revealed that guanidinylated chitosan is a promising candidate as an effective nonviral vector for in vivo gene delivery. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci, 2011

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