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Formulation and Characterization of Bioactive Agent Containing Nanodisks
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Epicatechin-Loaded Nanocapsules: Development, Physicochemical Characterization, and NLRP3 Inflammasome-Targeting

Carolina Bordin Davidson1,2, Éricles Forrati Machado1,3, Amanda Kolinski Machado2

  • 1Graduate Program in Nanosciences, Franciscan University, Santa Maria 97010-030, Brazil.

Biology
|November 27, 2025
PubMed
Summary

Epicatechin nanocapsules (NC-ECs) were developed to enhance anti-inflammatory effects. The formulation effectively modulated the NLRP3 inflammasome, showing promise for treating inflammatory diseases.

Keywords:
bioactive moleculeepicatechinflavonoidsinflammationnanocapsulenanotechnology

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Area of Science:

  • Nanomedicine
  • Pharmacology
  • Materials Science

Background:

  • Epicatechin, a flavonoid, has anti-inflammatory properties but suffers from poor bioavailability.
  • Flavonoids' therapeutic potential is limited by chemical instability, low solubility, and poor absorption.
  • The NLRP3 inflammasome is a key target for treating inflammatory conditions.

Purpose of the Study:

  • To encapsulate epicatechin into nanocapsules (NC-ECs) to improve its physicochemical properties and bioavailability.
  • To evaluate the anti-inflammatory efficacy of epicatechin nanocapsules via NLRP3 inflammasome modulation.
  • To assess the cytocompatibility and stability of the developed nanocapsule formulation.

Main Methods:

  • Epicatechin was encapsulated into Eudragit L-100 nanocapsules (NC-ECs) using interfacial polymer deposition.
  • Formulations were characterized for particle size, zeta potential, pH, encapsulation efficiency (HPLC), and morphology (AFM).
  • Cytocompatibility was tested on VERO cells, and anti-inflammatory activity was assessed in LPS + nigericin-stimulated THP-1 macrophages.

Main Results:

  • NC-ECs exhibited favorable physicochemical properties, high encapsulation efficiency (96%), and complete drug loading.
  • The nanocapsule formulation demonstrated good cytocompatibility with VERO cells.
  • NC-ECs preserved epicatechin's anti-inflammatory activity by modulating the NLRP3 inflammasome at low concentrations.

Conclusions:

  • Epicatechin-loaded nanocapsules (NC-ECs) represent a viable nanotechnological strategy for enhancing therapeutic applications.
  • NC-ECs show potential for treating inflammatory diseases associated with NLRP3 inflammasome activation.
  • This formulation contributes to the field of nanomedicine for inflammatory condition management.