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Issue 7, 2016
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Highly efficient siRNA delivery from core–shell mesoporous silica nanoparticles with multifunctional polymer caps

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Abstract

A new general route for siRNA delivery is presented combining porous core–shell silica nanocarriers with a modularly designed multifunctional block copolymer. Specifically, the internal storage and release of siRNA from mesoporous silica nanoparticles (MSN) with orthogonal core–shell surface chemistry was investigated as a function of pore-size, pore morphology, surface properties and pH. Very high siRNA loading capacities of up to 380 μg per mg MSN were obtained with charge-matched amino-functionalized mesoporous cores, and release profiles show up to 80% siRNA elution after 24 h. We demonstrate that adsorption and desorption of siRNA is mainly driven by electrostatic interactions, which allow for high loading capacities even in medium-sized mesopores with pore diameters down to 4 nm in a stellate pore morphology. The negatively charged MSN shell enabled the association with a block copolymer containing positively charged artificial amino acids and oleic acid blocks, which acts simultaneously as capping and endosomal release agent. The potential of this multifunctional delivery platform is demonstrated by highly effective cell transfection and siRNA delivery into KB-cells. A luciferase reporter gene knock-down of up to 80–90% was possible using extremely low cell exposures with only 2.5 μg MSN containing 0.5 μg siRNA per 100 μL well.

Graphical abstract: Highly efficient siRNA delivery from core–shell mesoporous silica nanoparticles with multifunctional polymer caps

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Publication details

The article was received on 10 Sep 2015, accepted on 29 Dec 2015 and first published on 30 Dec 2015


Article type: Paper
DOI: 10.1039/C5NR06246B
Citation: Nanoscale, 2016,8, 4007-4019
  • Open access: Creative Commons BY-NC license
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    Highly efficient siRNA delivery from core–shell mesoporous silica nanoparticles with multifunctional polymer caps

    K. Möller, K. Müller, H. Engelke, C. Bräuchle, E. Wagner and T. Bein, Nanoscale, 2016, 8, 4007
    DOI: 10.1039/C5NR06246B

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