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In Vitro Characterization, Modelling, and Antioxidant Properties of Polyphenon-60 from Green Tea in Eudragit S100-2 Chitosan Microspheres

Eudragit S100-coated chitosan microspheres (S100Ch) are proposed as a new oral delivery system for green tea polyphenon-60 (PP60). PP60 is a mixture of polyphenolic compounds, known for its active role in decreasing oxidative stress and metabolic risk factors involved in diabetes and in other chroni...

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Autores principales: Souto, Eliana B., da Ana, Raquel, Souto, Selma B., Zielińska, Aleksandra, Marques, Conrado, Andrade, Luciana N., Horbańczuk, Olaf K., Atanasov, Atanas G., Lucarini, Massimo, Durazzo, Alessandra, Silva, Amélia M., Novellino, Ettore, Santini, Antonello, Severino, Patricia
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7230985/
https://www.ncbi.nlm.nih.gov/pubmed/32244441
http://dx.doi.org/10.3390/nu12040967
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author Souto, Eliana B.
da Ana, Raquel
Souto, Selma B.
Zielińska, Aleksandra
Marques, Conrado
Andrade, Luciana N.
Horbańczuk, Olaf K.
Atanasov, Atanas G.
Lucarini, Massimo
Durazzo, Alessandra
Silva, Amélia M.
Novellino, Ettore
Santini, Antonello
Severino, Patricia
author_facet Souto, Eliana B.
da Ana, Raquel
Souto, Selma B.
Zielińska, Aleksandra
Marques, Conrado
Andrade, Luciana N.
Horbańczuk, Olaf K.
Atanasov, Atanas G.
Lucarini, Massimo
Durazzo, Alessandra
Silva, Amélia M.
Novellino, Ettore
Santini, Antonello
Severino, Patricia
author_sort Souto, Eliana B.
collection PubMed
description Eudragit S100-coated chitosan microspheres (S100Ch) are proposed as a new oral delivery system for green tea polyphenon-60 (PP60). PP60 is a mixture of polyphenolic compounds, known for its active role in decreasing oxidative stress and metabolic risk factors involved in diabetes and in other chronic diseases. Chitosan-PP60 microspheres prepared by an emulsion cross-linking method were coated with Eudragit S100 to ensure the release of PP60 in the terminal ileum. Different core–coat ratios of Eudragit and chitosan were tested. Optimized chitosan microspheres were obtained with a chitosan:PP60 ratio of 8:1 (Ch-PP60(8:1)), rotation speed of 1500 rpm, and surfactant concentration of 1.0% (m/v) achieving a mean size of 7.16 µm. Their coating with the enteric polymer (S100Ch-PP60) increased the mean size significantly (51.4 µm). The in vitro modified-release of PP60 from S100Ch-PP60 was confirmed in simulated gastrointestinal conditions. Mathematical fitting models were used to characterize the release mechanism showing that both Ch-PP60(8:1) and S100Ch-PP60 fitted the Korsmeyers–Peppas model. The antioxidant activity of PP60 was kept in glutaraldehyde-crosslinked chitosan microspheres before and after their coating, showing an IC(50) of 212.3 µg/mL and 154.4 µg/mL, respectively. The potential of chitosan microspheres for the delivery of catechins was illustrated, with limited risk of cytotoxicity as shown in Caco-2 cell lines using the 3-(4,5-dimethylthiazole-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The beneficial effects of green tea and its derivatives in the management of metabolic disorders can be exploited using mucoadhesive chitosan microspheres coated with enteric polymers for colonic delivery.
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spelling pubmed-72309852020-05-22 In Vitro Characterization, Modelling, and Antioxidant Properties of Polyphenon-60 from Green Tea in Eudragit S100-2 Chitosan Microspheres Souto, Eliana B. da Ana, Raquel Souto, Selma B. Zielińska, Aleksandra Marques, Conrado Andrade, Luciana N. Horbańczuk, Olaf K. Atanasov, Atanas G. Lucarini, Massimo Durazzo, Alessandra Silva, Amélia M. Novellino, Ettore Santini, Antonello Severino, Patricia Nutrients Article Eudragit S100-coated chitosan microspheres (S100Ch) are proposed as a new oral delivery system for green tea polyphenon-60 (PP60). PP60 is a mixture of polyphenolic compounds, known for its active role in decreasing oxidative stress and metabolic risk factors involved in diabetes and in other chronic diseases. Chitosan-PP60 microspheres prepared by an emulsion cross-linking method were coated with Eudragit S100 to ensure the release of PP60 in the terminal ileum. Different core–coat ratios of Eudragit and chitosan were tested. Optimized chitosan microspheres were obtained with a chitosan:PP60 ratio of 8:1 (Ch-PP60(8:1)), rotation speed of 1500 rpm, and surfactant concentration of 1.0% (m/v) achieving a mean size of 7.16 µm. Their coating with the enteric polymer (S100Ch-PP60) increased the mean size significantly (51.4 µm). The in vitro modified-release of PP60 from S100Ch-PP60 was confirmed in simulated gastrointestinal conditions. Mathematical fitting models were used to characterize the release mechanism showing that both Ch-PP60(8:1) and S100Ch-PP60 fitted the Korsmeyers–Peppas model. The antioxidant activity of PP60 was kept in glutaraldehyde-crosslinked chitosan microspheres before and after their coating, showing an IC(50) of 212.3 µg/mL and 154.4 µg/mL, respectively. The potential of chitosan microspheres for the delivery of catechins was illustrated, with limited risk of cytotoxicity as shown in Caco-2 cell lines using the 3-(4,5-dimethylthiazole-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The beneficial effects of green tea and its derivatives in the management of metabolic disorders can be exploited using mucoadhesive chitosan microspheres coated with enteric polymers for colonic delivery. MDPI 2020-03-31 /pmc/articles/PMC7230985/ /pubmed/32244441 http://dx.doi.org/10.3390/nu12040967 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
Souto, Eliana B.
da Ana, Raquel
Souto, Selma B.
Zielińska, Aleksandra
Marques, Conrado
Andrade, Luciana N.
Horbańczuk, Olaf K.
Atanasov, Atanas G.
Lucarini, Massimo
Durazzo, Alessandra
Silva, Amélia M.
Novellino, Ettore
Santini, Antonello
Severino, Patricia
In Vitro Characterization, Modelling, and Antioxidant Properties of Polyphenon-60 from Green Tea in Eudragit S100-2 Chitosan Microspheres
title In Vitro Characterization, Modelling, and Antioxidant Properties of Polyphenon-60 from Green Tea in Eudragit S100-2 Chitosan Microspheres
title_full In Vitro Characterization, Modelling, and Antioxidant Properties of Polyphenon-60 from Green Tea in Eudragit S100-2 Chitosan Microspheres
title_fullStr In Vitro Characterization, Modelling, and Antioxidant Properties of Polyphenon-60 from Green Tea in Eudragit S100-2 Chitosan Microspheres
title_full_unstemmed In Vitro Characterization, Modelling, and Antioxidant Properties of Polyphenon-60 from Green Tea in Eudragit S100-2 Chitosan Microspheres
title_short In Vitro Characterization, Modelling, and Antioxidant Properties of Polyphenon-60 from Green Tea in Eudragit S100-2 Chitosan Microspheres
title_sort in vitro characterization, modelling, and antioxidant properties of polyphenon-60 from green tea in eudragit s100-2 chitosan microspheres
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7230985/
https://www.ncbi.nlm.nih.gov/pubmed/32244441
http://dx.doi.org/10.3390/nu12040967
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