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Targeted delivery of siRNA using RGDfC-conjugated functionalized selenium nanoparticles for anticancer therapy

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Abstract

Lack of biocompatible and effective delivery carriers is a significant shortcoming for siRNA-mediated cancer therapy. To overcome these limitations, selenium nanoparticles (SeNPs) have been proposed for siRNA transfection vehicles. In this study, we synthesized novel RGDfC peptide modified selenium nanoparticles (RGDfC-SeNPs) as a gene vehicle, which was expected to improve the tumor-targeted delivery activity. RGDfC-SeNPs were compacted with siRNAs (anti-Oct4) by electrostatic interaction, which was capable of protecting siRNA from degradation. RGDfC-SeNPs exhibited excellent ability to deliver siRNA into HepG2 cells. siRNA transfection assay showed that RGDfC-SeNPs presented a higher gene silencing efficacy than conventional lipofectamine 2000. The cytotoxicity of RGDfC-SeNPs/siRNA on normal cells was lower than that on tumor cells, indicating that RGDfC-SeNPs/siRNA exhibited selectivity between normal and cancer cells. Additionally, Oct4 knockdown mediated by the selenium nanoparticle transfection arrested HepG2 cells mainly at the G2/M phase and significantly induced HepG2 cell apoptosis. Western blotting results showed that RGDfC-SeNPs/siRNA might trigger Wnt/β-catenin signaling, and further activate a BCL-2 apoptosis-related signaling pathway to advance HepG2 cell apoptosis. In vivo biodistribution experiments indicated that RGDfC-SeNPs/siRNA nanoparticles were specifically targeted to the HepG2 tumors. Most importantly, RGDfC-SeNPs/siRNA inhibited tumor growth significantly and induced HepG2 cell apoptosis via silencing the Oct4 gene. In addition, the results of H&E staining demonstrated that RGDfC-SeNPs/siRNA had negligible toxicity on the major organs of mice. In a word, this study provides a novel strategy for the design of biocompatible and effective siRNA delivery vehicles in cancer therapy.

Graphical abstract: Targeted delivery of siRNA using RGDfC-conjugated functionalized selenium nanoparticles for anticancer therapy

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Publication details

The article was received on 14 May 2017, accepted on 21 Jul 2017 and first published on 24 Jul 2017


Article type: Paper
DOI: 10.1039/C7TB01315A
Citation: J. Mater. Chem. B, 2017, Advance Article
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    Targeted delivery of siRNA using RGDfC-conjugated functionalized selenium nanoparticles for anticancer therapy

    Y. Xia, Z. Lin, Y. Li, M. Zhao, C. Wang, M. Guo, B. Zhang and B. Zhu, J. Mater. Chem. B, 2017, Advance Article , DOI: 10.1039/C7TB01315A

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