Research Article

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2017, 10(2): 503–519

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https://doi.org/10.1007/s12274-016-1309-1

Highly efficient gene silencing and bioimaging based on fluorescent carbon dots in vitro and in vivo

Seongchan Kim1,§, Yuri Choi2,§, Ginam Park3, Cheolhee Won3, Young-Joon Park4, Younghoon Lee5 (*), Byeong-Su Kim2 (*), and Dal-Hee Min1,3 (*)

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1 Center for RNA Research, Institute for Basic Sciences (IBS), Department of Chemistry, Seoul National University, Seoul 08826, Republic of Korea
2 Department of Energy Engineering and Department of Chemistry, Ulsan National Institute of Science and Technology (UNIST), Ulsan 44919, Republic of Korea
3 Institute of Nanobio Convergence Technology, Lemonex Inc., Seoul 08826, Republic of Korea
4 College of Pharmacy, Ajou University, Worldcuplo 206, Yeongtong-gu, Suwon 16499, Republic of Korea
5 Department of Chemistry, Korea Advanced Institute of Science and Technology (KAIST), Daejeon 34141, Republic of Korea
§ These authors contributed equally to this work.

Keywords: bioimaging, carbon dot, gene delivery, RNA interference, targeted cancer therapy
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ABSTRACT Small interfering RNA (siRNA) is an attractive therapeutic candidate for sequencespecific gene silencing to treat incurable diseases using small molecule drugs. However, its efficient intracellular delivery has remained a challenge. Here, we have developed a highly biocompatible fluorescent carbon dot (CD), and demonstrate a functional siRNA delivery system that induces efficient gene knockdown in vitro and in vivo. We found that CD nanoparticles (NPs) enhance the cellular uptake of siRNA, via endocytosis in tumor cells, with low cytotoxicity and unexpected immune responses. Real-time study of fluorescence imaging in live cells shows that CD NPs favorably localize in cytoplasm and successfully release siRNA within 12 h. Moreover, we demonstrate that CD NP-mediated siRNA delivery significantly silences green fluorescence protein (GFP) expression and inhibits tumor growth in a breast cancer cell xenograft mouse model of tumor-specific therapy. We have developed a multifunctional siRNA delivery vehicle enabling simultaneous bioimaging and efficient downregulation of gene expression, that shows excellent potential for gene therapy.
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Highly efficient gene silencing and bioimaging based on fluorescent carbon dots in vitro and in vivo. Nano Res. 2017, 10(2): 503–519 https://doi.org/10.1007/s12274-016-1309-1

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