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Open AccessFeature PaperArticle

Enhancing the Cellular Uptake and Antibacterial Activity of Rifampicin through Encapsulation in Mesoporous Silica Nanoparticles

1
Department of Physics, Chalmers University of Technology, SE-412 96 Gothenburg, Sweden
2
School of Pharmacy & Medical Sciences, University of South Australia, Adelaide, South Australia 5090, Australia
3
ARC Centre of Excellence in Bio-Nano Science and Technology, University of South Australia, Adelaide, South Australia 5090, Australia
*
Author to whom correspondence should be addressed.
Nanomaterials 2020, 10(4), 815; https://doi.org/10.3390/nano10040815
Received: 26 March 2020 / Revised: 18 April 2020 / Accepted: 20 April 2020 / Published: 24 April 2020
(This article belongs to the Special Issue Nanomedicine in Drug Delivery)
An urgent demand exists for the development of novel delivery systems that efficiently transport antibacterial agents across cellular membranes for the eradication of intracellular pathogens. In this study, the clinically relevant poorly water-soluble antibiotic, rifampicin, was confined within mesoporous silica nanoparticles (MSN) to investigate their ability to serve as an efficacious nanocarrier system against small colony variants of Staphylococcus aureus (SCV S. aureus) hosted within Caco-2 cells. The surface chemistry and particle size of MSN were varied through modifications during synthesis, where 40 nm particles with high silanol group densities promoted enhanced cellular uptake. Extensive biophysical analysis was performed, using quartz crystal microbalance with dissipation (QCM-D) and total internal reflection fluorescence (TIRF) microscopy, to elucidate the mechanism of MSN adsorption onto semi-native supported lipid bilayers (snSLB) and, thus, uncover potential cellular uptake mechanisms of MSN into Caco-2 cells. Such studies revealed that MSN with reduced silanol group densities were prone to greater particle aggregation on snSLB, which was expected to restrict endocytosis. MSN adsorption and uptake into Caco-2 cells correlated well with antibacterial efficacy against SCV S. aureus, with 40 nm hydrophilic particles triggering a ~2.5-log greater reduction in colony forming units, compared to the pure rifampicin. Thus, this study provides evidence for the potential to design silica nanocarrier systems with controlled surface chemistries that can be used to re-sensitise intracellular bacteria to antibiotics by delivering them to the site of infection. View Full-Text
Keywords: mesoporous silica; nanoparticle; permeability; antibiotics; total internal reflection; fluorescence microscopy; Caco-2; infection; small colony variants; Staphylococcus aureus mesoporous silica; nanoparticle; permeability; antibiotics; total internal reflection; fluorescence microscopy; Caco-2; infection; small colony variants; Staphylococcus aureus
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MDPI and ACS Style

Joyce, P.; Ulmefors, H.; Maghrebi, S.; Subramaniam, S.; Wignall, A.; Jõemetsa, S.; Höök, F.; Prestidge, C.A. Enhancing the Cellular Uptake and Antibacterial Activity of Rifampicin through Encapsulation in Mesoporous Silica Nanoparticles. Nanomaterials 2020, 10, 815.

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