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Development, Optimization and Characterization of Eudraguard®-based Microparticles for Colon Delivery.

Claudia Curcio1, Antonio S Greco1, Salvatore Rizzo1

  • 1Department of Drug Sciences, Section of Pharmaceutical Technology, University of Catania, 95125 Catania, Italy.

Pharmaceuticals (Basel, Switzerland)
|July 1, 2020
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Summary

This study developed pH-dependent microparticles using Eudraguard® Biotic and Eudraguard® Control for colon delivery of quercetin. The emulsion-solvent evaporation method yielded optimal systems with limited gastric release and good colonic release.

Keywords:
DSCFT-IRPXRDdrug deliveryenteric releasefood-grade acrylate polymersquercetin

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Area of Science:

  • Pharmaceutical Sciences
  • Materials Science
  • Nutraceuticals

Background:

  • Developing pH-dependent systems for colon delivery of natural active ingredients is crucial for nutraceutical products.
  • Eudraguard® resins (methacrylate copolymers) are food-grade polymers suitable for food supplements.
  • Eudraguard® Biotic (EUG-B) offers pH-dependent solubility, while Eudraguard® Control (EUG-C) provides prolonged release.

Purpose of the Study:

  • To optimize microparticle preparation techniques for Eudraguard® resins.
  • To evaluate the encapsulation and specific colonic release of quercetin (QUE) using EUG-B and EUG-C.
  • To assess the in vitro release profiles simulating gastrointestinal tract pH variations.

Main Methods:

  • Preparation of unloaded and quercetin-loaded Eudraguard® microparticles using various techniques.
  • Solid-state characterization including FT-IR spectroscopy, differential scanning calorimetry, and X-ray diffractometry.
  • In vitro drug release studies simulating physiological pH changes in the gastrointestinal tract.

Main Results:

  • The emulsion-solvent evaporation method, without an aqueous phase, produced the best microparticle systems.
  • Solid-state analysis confirmed uniform dispersion of quercetin in a non-crystalline state within the polymer matrix.
  • In vitro tests demonstrated limited quercetin release in simulated gastric conditions and significant release in simulated colonic conditions.

Conclusions:

  • Eudraguard® Biotic and Eudraguard® Control microparticles are effective for colon-specific delivery of quercetin.
  • The emulsion-solvent evaporation method is optimal for preparing these microparticle systems.
  • These findings support the potential of Eudraguard® resins in developing advanced nutraceutical delivery systems.