Quercetin-Loaded Nanoparticles: A Promising Therapeutic Strategy for Inflammatory Bowel Disease

Area of Science:

• Nanotechnology
• Pharmacology
• Gastroenterology

Background:

• Inflammatory bowel disease (IBD) poses a significant health challenge, necessitating novel therapeutic strategies.
• Quercetin, a natural flavonoid, exhibits anti-inflammatory properties but suffers from poor bioavailability.
• Nanoparticle-based drug delivery systems offer a promising approach to enhance quercetin's therapeutic potential for IBD.

Purpose of the Study:

• To develop and characterize quercetin-loaded nanoparticles (NPs) using poly lactic-co-glycolic acid (PLGA) and Eudragit S100 (ES100).
• To evaluate the in vitro and in vivo therapeutic efficacy of these quercetin-loaded NPs in preclinical models of inflammatory bowel disease (IBD).

Main Methods:

• Quercetin-loaded NPs (QU-PLGA and QU-PE) were prepared and characterized for particle size, encapsulation efficiency, and stability.
• In vitro studies assessed cell uptake and cytotoxicity in Caco-2 and SW480 cells.
• In vivo efficacy was evaluated in dextran sulfate sodium (DSS) and oxazolone (OXA) induced acute colitis models in mice, measuring disease severity and inflammatory markers.

Main Results:

• Quercetin-loaded NPs exhibited significantly smaller particle sizes and high encapsulation efficiencies compared to free quercetin.
• QU-PE demonstrated pH-dependent release and improved stability, while both NP formulations showed enhanced cell penetration and were non-toxic.
• In vivo studies revealed that quercetin-loaded NPs significantly reduced colitis severity, improved disease markers, and modulated inflammatory responses, with QU-PE showing consistent effects and QU-PLGA performing well in the DSS model.

Conclusions:

• Quercetin-loaded nanoparticles enhance quercetin's stability, bioavailability, and therapeutic efficacy for inflammatory bowel disease (IBD).
• These NP formulations represent a promising and physiologically relevant therapeutic strategy for managing colitis.
• The study highlights the potential of PLGA and ES100 as effective carriers for quercetin delivery in IBD treatment.