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Synthesis and characterization of dexamethasone-conjugated linear polyethylenimine as a gene carrier

Authors

  • Hyunjung Kim,

    1. Department of Bioengineering, College of Engineering, Hanyang University, Seoul 133-791, Korea
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  • Yun Mi Bae,

    1. Department of Biochemistry, College of Natural Sciences, Chungnam National University, Daejeon 305-764, Korea
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  • Hyun Ah Kim,

    1. Department of Bioengineering, College of Engineering, Hanyang University, Seoul 133-791, Korea
    2. Institute for Bioengineering and Biopharmaceutical Research, Hanyang University, Seoul 133-791, Korea
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  • Hyesun Hyun,

    1. Department of Bioengineering, College of Engineering, Hanyang University, Seoul 133-791, Korea
    2. Institute for Bioengineering and Biopharmaceutical Research, Hanyang University, Seoul 133-791, Korea
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  • Gwang Sig Yu,

    1. Department of Biochemistry, College of Natural Sciences, Chungnam National University, Daejeon 305-764, Korea
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  • Joon Sig Choi,

    1. Department of Biochemistry, College of Natural Sciences, Chungnam National University, Daejeon 305-764, Korea
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  • Minhyung Lee

    Corresponding author
    1. Department of Bioengineering, College of Engineering, Hanyang University, Seoul 133-791, Korea
    2. Institute for Bioengineering and Biopharmaceutical Research, Hanyang University, Seoul 133-791, Korea
    • Department of Bioengineering, College of Engineering, Hanyang University, 17 Haengdang-dong, Seongdong-gu, Seoul 133-791, Korea.
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Abstract

Linear polyethylenimine (25 kDa, LPEI25k) has been shown to be an effective non-viral gene carrier with higher transfection and lower toxicity than branched polyethylenimine (BPEI) of comparable molecular weight. In this study, dexamethasone was conjugated to LPEI25k to improve the efficiency of gene delivery. Dexamethasone is a synthetic glucocorticoid receptor ligand. Dexamethasone-conjugated LPEI25k (LPEI–Dexa) was evaluated as a gene carrier in various cells. Gel retardation assays showed that LPEI–Dexa completely retarded plasmid DNA (pDNA) at a 0.75:1 weight ratio (LPEI/pDNA). LPEI–Dexa had the highest transfection efficiency at a 2:1 weight ratio (LPEI–Dexa/DNA). At this ratio, the size of the LPEI–Dexa/pDNA complex was approximately 125 nm and the zeta potential was 35 mV. LPEI–Dexa had higher transfection efficiency than LPEI and Lipofectamine 2000. In addition, the cytotoxicity of LPEI–Dexa was much lower than that of BPEI (25 kDa, BPEI25k). In conclusion, LPEI–Dexa has a high transfection efficiency and low toxicity and can therefore be used for non-viral gene delivery. J. Cell. Biochem. 110: 743–751, 2010. © 2010 Wiley-Liss, Inc.

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