Modulation of Inflammatory Mediators by Polymeric Nanoparticles Loaded with Anti-Inflammatory Drugs

نویسندگان

چکیده

The first-line treatment of osteoarthritis is based on anti-inflammatory drugs, the most currently used being nonsteroidal selective cyclooxygenase 2 (COX-2) inhibitors and corticoids. Most them present cytotoxicity low bioavailability in physiological conditions, making necessary administration high drug concentrations causing several side effects. goal this work was to encapsulate three hydrophobic drugs different natures (celecoxib, tenoxicam dexamethasone) into core-shell terpolymer nanoparticles with potential applications osteoarthritis. Nanoparticles presented hydrodynamic diameters between 110 130 nm almost neutral surface charges (between −1 −5 mV). Encapsulation efficiencies were highly dependent loaded its water solubility, having higher values for celecoxib (39–72%) followed by (20–24%) dexamethasone (14–26%). Nanoencapsulation reduced human articular chondrocytes murine RAW264.7 macrophages. Moreover, systems did not show cytotoxic effects a wide range concentrations. Celecoxib dexamethasone-loaded release inflammatory mediators (NO, TNF-α, IL-1β, IL-6, PGE2 IL-10) lipopolysaccharide (LPS)-stimulated RAW264.7. Tenoxicam-loaded NO production, although an overexpression IL-6 IL-10 observed. Finally, all proved be biocompatible subcutaneous injection model rats. These findings suggest that these could suitable candidates processes associated due their demonstrated vitro activity as regulators mediator production.

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ژورنال

عنوان ژورنال: Pharmaceutics

سال: 2021

ISSN: ['1999-4923']

DOI: https://doi.org/10.3390/pharmaceutics13020290