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Empowering Naringin's Anti-Inflammatory Effects through Nanoencapsulation.

Andreia Marinho1,2, Catarina Leal Seabra1, Sofia A C Lima3

  • 1LAQV, REQUIMTE, Faculdade de Farmácia, Universidade do Porto, R. Jorge de Viterbo Ferreira 228, 4050-313 Porto, Portugal.

International Journal of Molecular Sciences
|April 27, 2024
PubMed
Summary

This study developed lipid nanoparticles (LNPs) to improve the anti-inflammatory effects of naringin (NAR). The new formulation enhanced NAR delivery to inflamed tissues, showing significant potential for treating inflammatory conditions.

Keywords:
anti-inflammatory activityhyaluronic acidlipid nanoparticlesmacrophagesnaringin

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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@NPsHA).

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@NPsHA 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@NPsHA 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@NPsHA show promise for targeted therapy of inflammatory diseases by modulating key inflammatory mediators.