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Article

Cylindrical Microparticles Composed of Mesoporous Silica Nanoparticles for the Targeted Delivery of a Small Molecule and a Macromolecular Drug to the Lungs: Exemplified with Curcumin and siRNA

1
Department of Pharmacy, Biopharmaceutics and Pharmaceutical Technology, Saarland University, Campus C4 1, 66123 Saarbruecken, Germany
2
INM-Leibniz Institute for New Materials, Campus D2 2, 66123 Saarbruecken, Germany
*
Author to whom correspondence should be addressed.
Academic Editor: Korbinian Löbmann
Pharmaceutics 2021, 13(6), 844; https://doi.org/10.3390/pharmaceutics13060844
Received: 14 May 2021 / Revised: 1 June 2021 / Accepted: 2 June 2021 / Published: 7 June 2021
(This article belongs to the Special Issue Advances in Pulmonary Drug Delivery, Volume II)
The transport of macromolecular drugs such as oligonucleotides into the lungs has become increasingly relevant in recent years due to their high potency. However, the chemical structure of this group of drugs poses a hurdle to their delivery, caused by the negative charge, membrane impermeability and instability. For example, siRNA to reduce tumour necrosis factor alpha (TNF-α) secretion to reduce inflammatory signals has been successfully delivered by inhalation. In order to increase the effect of the treatment, a co-transport of another anti-inflammatory ingredient was applied. Combining curcumin-loaded mesoporous silica nanoparticles in nanostructured cylindrical microparticles stabilized by the layer-by-layer technique using polyanionic siRNA against TNF-α was used for demonstration. This system showed aerodynamic properties suited for lung deposition (mass median aerodynamic diameter of 2.85 ± 0.44 µm). Furthermore, these inhalable carriers showed no acute in vitro toxicity tested in both alveolar epithelial cells and macrophages up to 48 h incubation. Ultimately, TNF-α release was significantly reduced by the particles, showing an improved activity co-delivering both drugs using such a drug-delivery system for specific inhibition of TNF-α in the lungs. View Full-Text
Keywords: nanotechnology; pulmonary delivery; TNFalpha inhibition; RNA release; inhalation therapy; aspheric drug delivery systems; curcumin delivery; synergistic effect nanotechnology; pulmonary delivery; TNFalpha inhibition; RNA release; inhalation therapy; aspheric drug delivery systems; curcumin delivery; synergistic effect
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MDPI and ACS Style

Fischer, T.; Winter, I.; Drumm, R.; Schneider, M. Cylindrical Microparticles Composed of Mesoporous Silica Nanoparticles for the Targeted Delivery of a Small Molecule and a Macromolecular Drug to the Lungs: Exemplified with Curcumin and siRNA. Pharmaceutics 2021, 13, 844. https://doi.org/10.3390/pharmaceutics13060844

AMA Style

Fischer T, Winter I, Drumm R, Schneider M. Cylindrical Microparticles Composed of Mesoporous Silica Nanoparticles for the Targeted Delivery of a Small Molecule and a Macromolecular Drug to the Lungs: Exemplified with Curcumin and siRNA. Pharmaceutics. 2021; 13(6):844. https://doi.org/10.3390/pharmaceutics13060844

Chicago/Turabian Style

Fischer, Thorben, Inga Winter, Robert Drumm, and Marc Schneider. 2021. "Cylindrical Microparticles Composed of Mesoporous Silica Nanoparticles for the Targeted Delivery of a Small Molecule and a Macromolecular Drug to the Lungs: Exemplified with Curcumin and siRNA" Pharmaceutics 13, no. 6: 844. https://doi.org/10.3390/pharmaceutics13060844

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