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Open AccessArticle

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

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Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Coimbra, Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal
2
CEB—Centre of Biological Engineering, University of Minho, Campus de Gualtar, 4710-057 Braga, Portugal
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Department of Endocrinology, Hospital de São João, Alameda Prof. Hernâni Monteiro, 4200-319 Porto, Portugal
4
Laboratory of Nanotechnology and Nanomedicine (LNMED), Institute of Technology and Research (ITP), Av. Murilo Dantas, 300, Aracaju 49010-390, Brazil
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Industrial Biotechnology Program, University of Tiradentes (UNIT), Av. Murilo Dantas 300, Aracaju 49032-490, Brazil
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Tiradentes Institute, 150 Mt Vernon St, Dorchester, MA 02125, USA
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Department of Physiology, Federal University of Sergipe, CEP São Cristóvão 49100-000, Sergipe, Brazil
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Department of Technique and Food Product Development, Warsaw University of Life Sciences (WULS-SGGW) 159c Nowoursynowska, 02-776 Warsaw, Poland
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The Institute of Genetics and Animal Breeding, Polish Academy of Sciences, Jastrzębiec, 05-552 Magdalenka, Poland
10
Institute of Neurobiology, Bulgarian Academy of Sciences, 23 Acad. G. Bonchev str., 1113 Sofia, Bulgaria
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Department of Pharmacognosy, University of Vienna, 1090 Vienna, Austria
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Ludwig Boltzmann Institute for Digital Health and Patient Safety, Medical University of Vienna, Spitalgasse 23, 1090 Vienna, Austria
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CREA-Research Centre for Food and Nutrition, Via Ardeatina 546, 00178 Rome, Italy
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Department of Biology and Environment, University of Trás-os-Montes e Alto Douro (UTAD), Quinta de Prados, 5001-801 Vila Real, Portugal
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Centre for Research and Technology of Agro-Environmental and Biological Sciences (CITAB), University of Trás-os-Montes e Alto Douro (UTAD), 5001-801 Vila Real, Portugal
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Department of Pharmacy, University of Napoli Federico II, 80131 Napoli, Italy
*
Authors to whom correspondence should be addressed.
Nutrients 2020, 12(4), 967; https://doi.org/10.3390/nu12040967
Received: 27 February 2020 / Revised: 27 March 2020 / Accepted: 30 March 2020 / Published: 31 March 2020
(This article belongs to the Special Issue Diets, Foods and Food Components Effect on Dyslipidemia)
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-PP608:1), 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-PP608:1 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 IC50 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. View Full-Text
Keywords: green tea; epigallocatechin gallate; chitosan; microspheres; Eudragit; metabolic diseases green tea; epigallocatechin gallate; chitosan; microspheres; Eudragit; metabolic diseases
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MDPI and ACS Style

Souto, E.B.; da Ana, R.; Souto, S.B.; Zielińska, A.; Marques, C.; Andrade, L.N.; Horbańczuk, O.K.; Atanasov, A.G.; Lucarini, M.; Durazzo, A.; Silva, A.M.; Novellino, E.; Santini, A.; Severino, P. In Vitro Characterization, Modelling, and Antioxidant Properties of Polyphenon-60 from Green Tea in Eudragit S100-2 Chitosan Microspheres. Nutrients 2020, 12, 967. https://doi.org/10.3390/nu12040967

AMA Style

Souto EB, da Ana R, Souto SB, Zielińska A, Marques C, Andrade LN, Horbańczuk OK, Atanasov AG, Lucarini M, Durazzo A, Silva AM, Novellino E, Santini A, Severino P. In Vitro Characterization, Modelling, and Antioxidant Properties of Polyphenon-60 from Green Tea in Eudragit S100-2 Chitosan Microspheres. Nutrients. 2020; 12(4):967. https://doi.org/10.3390/nu12040967

Chicago/Turabian Style

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. 2020. "In Vitro Characterization, Modelling, and Antioxidant Properties of Polyphenon-60 from Green Tea in Eudragit S100-2 Chitosan Microspheres" Nutrients 12, no. 4: 967. https://doi.org/10.3390/nu12040967

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