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Cellular Delivery of siRNA Using Poly(2-dimethylaminoethyl methacrylate)- Functionalized Graphene Oxide Nano-Wrap

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Abstract

Despite its high therapeutic potential, the use of siRNA has still been limited mostly due to the lack of a proper delivery system. Small number of charges and inflexible structure of siRNA are the major factors that affect cellular delivery efficiency of conventional lipid and polymeric carriers. In this study, we synthesized a 2-dimensional (2D) carrier for siRNA using a facile method to functionalize and stabilize the surface of graphene oxide (GO) with catechol-derivatized poly(2-dimethylaminoethyl methacrylate) (C-p(DMAEMA)). The resulting GO/C-p(DMAEMA) can interact with siRNA on the flexible 2D surface of the GO, wrapping up siRNA molecules by folding to form a dim sum-like nano structure. GO/C-p(DMAEMA) demonstrated significantly improved cellular uptake and enhanced gene silencing efficiency in the presence of serum protein, compared to unmodified GO and bPEI 25 kDa.

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Correspondence to Sung Young Park or Ji Hoon Jeong.

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Acknowledgments: This research was supported by the National Research Foundation of Korea (NRF) grant (2016R1A2B4015056, 2017M3A9F5032628, 2010-0027955) funded by Ministry of Science and ICT (MSIT) and Basic Science Research Program (2018R1A6A1A03023788) through the National Research Foundation of Korea (NRF) funded by the Ministry of Education.

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Lee, J.E., Lee, K., Nam, J.A. et al. Cellular Delivery of siRNA Using Poly(2-dimethylaminoethyl methacrylate)- Functionalized Graphene Oxide Nano-Wrap. Macromol. Res. 26, 1115–1122 (2018). https://doi.org/10.1007/s13233-019-7017-4

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