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Development, Optimization and Characterization of Eudraguard(®)-Based Microparticles for Colon Delivery

Development of pH-dependent systems for colon delivery of natural active ingredients is an attractive area of research in the field of nutraceutical products. This study was focused on Eudraguard(®) resins, that are methacrylate copolymers approved as “food grade” by European Commission and useful f...

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Detalles Bibliográficos
Autores principales: Curcio, Claudia, Greco, Antonio S., Rizzo, Salvatore, Saitta, Lorena, Musumeci, Teresa, Ruozi, Barbara, Pignatello, Rosario
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7344638/
https://www.ncbi.nlm.nih.gov/pubmed/32599861
http://dx.doi.org/10.3390/ph13060131
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author Curcio, Claudia
Greco, Antonio S.
Rizzo, Salvatore
Saitta, Lorena
Musumeci, Teresa
Ruozi, Barbara
Pignatello, Rosario
author_facet Curcio, Claudia
Greco, Antonio S.
Rizzo, Salvatore
Saitta, Lorena
Musumeci, Teresa
Ruozi, Barbara
Pignatello, Rosario
author_sort Curcio, Claudia
collection PubMed
description Development of pH-dependent systems for colon delivery of natural active ingredients is an attractive area of research in the field of nutraceutical products. This study was focused on Eudraguard(®) resins, that are methacrylate copolymers approved as “food grade” by European Commission and useful for the production of food supplements. In particular, Eudraguard(®) Biotic (EUG-B), characterized by a pH-dependent solubility and Eudraguard(®) Control (EUG-C), whose chemical properties support a prolonged release of the encapsulated compounds, were tested. To obtain EUG microparticles, different preparation techniques were tested, in order to optimize the preparation method and observe the effect upon drug encapsulation and specific colonic release. Unloaded microparticles were initially produced to evaluate the influence of polymer characteristics on the formulation process; subsequently microparticles loaded with quercetin (QUE) as a low solubility model drug were prepared. The characterization of microparticles in the solid-state (FT-IR spectroscopy, differential scanning calorimetry and X-ray diffractometry) indicated that QUE was uniformly dispersed in a non-crystalline state in the polymeric network, without strong signs of chemical interactions. Finally, to assess the ability of EUG-C and EUG-B to control the drug release in the gastric environment, and to allow an increased release at a colonic level, suitable in vitro release tests were carried out by simulating the pH variations along the gastro-intestinal tract. Among the evaluated preparation methods, those in which an aqueous phase was not present, and in particular the emulsion-solvent evaporation method produced the best microparticle systems. The in vitro tests showed a limited drug release at a gastric level and a good specific colon release.
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spelling pubmed-73446382020-07-09 Development, Optimization and Characterization of Eudraguard(®)-Based Microparticles for Colon Delivery Curcio, Claudia Greco, Antonio S. Rizzo, Salvatore Saitta, Lorena Musumeci, Teresa Ruozi, Barbara Pignatello, Rosario Pharmaceuticals (Basel) Article Development of pH-dependent systems for colon delivery of natural active ingredients is an attractive area of research in the field of nutraceutical products. This study was focused on Eudraguard(®) resins, that are methacrylate copolymers approved as “food grade” by European Commission and useful for the production of food supplements. In particular, Eudraguard(®) Biotic (EUG-B), characterized by a pH-dependent solubility and Eudraguard(®) Control (EUG-C), whose chemical properties support a prolonged release of the encapsulated compounds, were tested. To obtain EUG microparticles, different preparation techniques were tested, in order to optimize the preparation method and observe the effect upon drug encapsulation and specific colonic release. Unloaded microparticles were initially produced to evaluate the influence of polymer characteristics on the formulation process; subsequently microparticles loaded with quercetin (QUE) as a low solubility model drug were prepared. The characterization of microparticles in the solid-state (FT-IR spectroscopy, differential scanning calorimetry and X-ray diffractometry) indicated that QUE was uniformly dispersed in a non-crystalline state in the polymeric network, without strong signs of chemical interactions. Finally, to assess the ability of EUG-C and EUG-B to control the drug release in the gastric environment, and to allow an increased release at a colonic level, suitable in vitro release tests were carried out by simulating the pH variations along the gastro-intestinal tract. Among the evaluated preparation methods, those in which an aqueous phase was not present, and in particular the emulsion-solvent evaporation method produced the best microparticle systems. The in vitro tests showed a limited drug release at a gastric level and a good specific colon release. MDPI 2020-06-24 /pmc/articles/PMC7344638/ /pubmed/32599861 http://dx.doi.org/10.3390/ph13060131 Text en © 2020 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Curcio, Claudia
Greco, Antonio S.
Rizzo, Salvatore
Saitta, Lorena
Musumeci, Teresa
Ruozi, Barbara
Pignatello, Rosario
Development, Optimization and Characterization of Eudraguard(®)-Based Microparticles for Colon Delivery
title Development, Optimization and Characterization of Eudraguard(®)-Based Microparticles for Colon Delivery
title_full Development, Optimization and Characterization of Eudraguard(®)-Based Microparticles for Colon Delivery
title_fullStr Development, Optimization and Characterization of Eudraguard(®)-Based Microparticles for Colon Delivery
title_full_unstemmed Development, Optimization and Characterization of Eudraguard(®)-Based Microparticles for Colon Delivery
title_short Development, Optimization and Characterization of Eudraguard(®)-Based Microparticles for Colon Delivery
title_sort development, optimization and characterization of eudraguard(®)-based microparticles for colon delivery
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7344638/
https://www.ncbi.nlm.nih.gov/pubmed/32599861
http://dx.doi.org/10.3390/ph13060131
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