Empowering Naringin's Anti-Inflammatory Effects through Nanoencapsulation

Area of Science:

• Pharmacology
• Nanotechnology
• Immunology

Background:

• Naringin (NAR), a citrus flavonoid, possesses anti-inflammatory properties but suffers from poor bioavailability due to extensive metabolism.
• Targeting drug delivery systems to inflamed tissues is crucial for enhancing therapeutic efficacy and minimizing side effects.

Purpose of the Study:

• To develop hyaluronic acid (HA)-functionalized lipid nanoparticles (LNPs) for targeted delivery of naringin (NAR) to CD44 receptors on activated macrophages.
• To evaluate the anti-inflammatory potential and efficacy of the developed NAR-loaded LNPs (NAR@NPs_HA).

Main Methods:

• Formulation of NAR-loaded LNPs functionalized with HA for CD44 receptor targeting.
• Characterization of nanoparticle size, polydispersity, loading capacity, and zeta potential.
• In vitro assessment of NAR release kinetics, cytocompatibility, hemolytic activity, and modulation of inflammatory mediators (TNF-α, CCL-3, IL-1β, IL-6).

Main Results:

• NAR@NPs_HA exhibited optimal physicochemical properties (size < 200 nm, PDI ~0.245, loading ~10%, zeta potential ~10 mV).
• In vitro studies demonstrated controlled NAR release, high cytocompatibility, and low hemolytic activity.
• NAR@NPs_HA significantly reduced inflammatory markers: TNF-α (80%), CCL-3 (90%), IL-1β (66%), and IL-6 (45%) in response to LPS stimulation.

Conclusions:

• Hyaluronic acid-functionalized lipid nanoparticles represent an effective drug delivery system for naringin, enhancing its anti-inflammatory effects.
• The developed NAR@NPs_HA show promise for targeted therapy of inflammatory diseases by modulating key inflammatory mediators.