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Small Interfering RNA Nunchucks with a Hydrophobic Linker for Efficient Intracellular Delivery

Authors

  • Sung Duk Jo,

    1. Department of Biological Sciences, Korea Advanced Institute of Science and Technology, Daejeon, Republic of Korea
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  • Jee Seon Kim,

    1. Department of Materials Science and Engineering, Korea Advanced Institute of Science and Technology, Daejeon, Republic of Korea
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  • Cheol O. Joe,

    1. Department of Biological Sciences, Korea Advanced Institute of Science and Technology, Daejeon, Republic of Korea
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  • Hyejung Mok,

    Corresponding author
    1. Department of Bioscience and Biotechnology, Konkuk University, Seoul, Republic of Korea
    • Hyejung Mok, Department of Bioscience and Biotechnology, Konkuk University, Seoul143-701Republic of Korea

      Yoon Sung Nam, Department of Biological Sciences, Korea Advanced Institute of Science and Technology, Daejeon305-701Republic of Korea

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  • Yoon Sung Nam

    Corresponding author
    1. Department of Biological Sciences, Korea Advanced Institute of Science and Technology, Daejeon, Republic of Korea
    2. Department of Materials Science and Engineering, Korea Advanced Institute of Science and Technology, Daejeon, Republic of Korea
    3. KAIST Institutes for NanoCentury and BioCentury, Korea Advanced Institute of Science and Technology, Daejeon, Republic of Korea
    • Hyejung Mok, Department of Bioscience and Biotechnology, Konkuk University, Seoul143-701Republic of Korea

      Yoon Sung Nam, Department of Biological Sciences, Korea Advanced Institute of Science and Technology, Daejeon305-701Republic of Korea

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  • Supporting Information is available from the Wiley Online Library or from the author.

Abstract

The high stiffness and low spatial charge density of siRNA limit the effectiveness of the electrostatic condensation of siRNA with cationic polyelectrolytes. Here, a facile method to stabilize nanoscale siRNA/polyelectrolyte complexes by introducing a reductively cleavable alkyl chain to siRNA as a hybrophobic linker of dimeric siRNA conjugates is reported. The increased length of the hydrophobic linker increases the intracellular translocation and gene silencing activity of the dimeric siRNA conjugates when they are complexed with linear polyethylenimine (LPEI). The results suggest that the introduction of a hydrophobic linker in the dimeric siRNA conjugates can facilitate the intracellular delivery of siRNA through effective condensation with cationic polyelectrolytes.mabi201300291-gra-0001

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