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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

  • 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

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Document Type:Article
Author:Thorben Fischer, Inga Winter, Robert Drumm, Marc SchneiderORCiD
Parent Title (English):Pharmaceutics
Year of first Publication:2021
Release Date:2022/11/18
Tag:RNA release; TNF alpha inhibition; aspheric drug delivery systems; curcumin delivery; inhalation therapy; nanotechnology; pulmonary delivery; syntergistic effect
Impact:06.525 (2021)
Funding Information:Mukoviszidose eV (WT/2-LFFP 17/081702)
Open Access:Open Access
Signature:INM 2021/073
Licence (German):License LogoCreative Commons - CC BY - Namensnennung 4.0 International