Simple Approach to Enhance Green Tea Epigallocatechin Gallate Stability in Aqueous Solutions and Bioavailability: Experimental and Theoretical Characterizations
Because of its antioxidant, antimutagenic, and anti-infectious properties, epigallocatechin gallate (EGCG) is the most interesting compound among the green tea catechins polyphenols. However, its health effects are inconclusive due to its very low bioavailability, largely due to a particular instabi...
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| Format: | Article |
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MDPI AG
2021-11-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/14/12/1242 |
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| author | Philippe-Henri Secretan Olivier Thirion Hassane Sadou Yayé Thibaud Damy Alain Astier Muriel Paul Bernard Do |
| author_facet | Philippe-Henri Secretan Olivier Thirion Hassane Sadou Yayé Thibaud Damy Alain Astier Muriel Paul Bernard Do |
| author_sort | Philippe-Henri Secretan |
| collection | DOAJ |
| description | Because of its antioxidant, antimutagenic, and anti-infectious properties, epigallocatechin gallate (EGCG) is the most interesting compound among the green tea catechins polyphenols. However, its health effects are inconclusive due to its very low bioavailability, largely due to a particular instability that does not allow EGCG to reach the potency required for clinical developments. Over the last decade, many efforts have been made to improve the stability and bioavailability of EGCG using complex delivery systems such as nanotechnology, but these efforts have not been successful and easy to translate to industrial use. To meet the needs of a large-scale clinical trial requiring EGCG in a concentrated solution to anticipate swallowing impairments, we developed an EGCG-based aqueous solution in the simplest way while trying to circumvent EGCG instability. The solution was thoroughly characterized to sort out the unexpected stability outcome by combining experimental (HPLC-UV-mass spectrometry and infrared spectroscopy) and computational (density functional theory) studies. Against all odds, the EGCG–sucrose complex under certain conditions may have prevented EGCG from degradation in aqueous media. Indeed, in agreement with the ICH guidelines, the formulated solution was shown to be stable up to at least 24 months under 2–8 °C and at ambient temperature. Furthermore, considerable improvement in bioavailability in rats, against EGCG powder formulated in hard-gel capsules, was shown after gavage. Thus, the proposed formulation may provide an easily implementable platform to administer EGCG in the context of clinical development. |
| first_indexed | 2024-03-10T03:21:10Z |
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| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-10T03:21:10Z |
| publishDate | 2021-11-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-1a52ae2200de42d7a80b59ceeebf4ddf2023-11-23T10:02:56ZengMDPI AGPharmaceuticals1424-82472021-11-011412124210.3390/ph14121242Simple Approach to Enhance Green Tea Epigallocatechin Gallate Stability in Aqueous Solutions and Bioavailability: Experimental and Theoretical CharacterizationsPhilippe-Henri Secretan0Olivier Thirion1Hassane Sadou Yayé2Thibaud Damy3Alain Astier4Muriel Paul5Bernard Do6Matériaux et Santé, Université Paris-Saclay, 92296 Châtenay-Malabry, FranceDepartment of Pharmacy, Hôpitaux Universitaires Henri Mondor, AP-HP, 94000 Créteil, FranceDepartment of Pharmacy, Hôpitaux Universitaires Pitié-Salpêtrière, AP-HP, 75013 Paris, FranceDépartement de Cardiologie et des Maladies Vasculaires, Hôpitaux Universitaires Henri Mondor, AP-HP, 94000 Créteil, FranceDepartment of Pharmacy, Hôpitaux Universitaires Henri Mondor, AP-HP, 94000 Créteil, FranceDepartment of Pharmacy, Hôpitaux Universitaires Henri Mondor, AP-HP, 94000 Créteil, FranceMatériaux et Santé, Université Paris-Saclay, 92296 Châtenay-Malabry, FranceBecause of its antioxidant, antimutagenic, and anti-infectious properties, epigallocatechin gallate (EGCG) is the most interesting compound among the green tea catechins polyphenols. However, its health effects are inconclusive due to its very low bioavailability, largely due to a particular instability that does not allow EGCG to reach the potency required for clinical developments. Over the last decade, many efforts have been made to improve the stability and bioavailability of EGCG using complex delivery systems such as nanotechnology, but these efforts have not been successful and easy to translate to industrial use. To meet the needs of a large-scale clinical trial requiring EGCG in a concentrated solution to anticipate swallowing impairments, we developed an EGCG-based aqueous solution in the simplest way while trying to circumvent EGCG instability. The solution was thoroughly characterized to sort out the unexpected stability outcome by combining experimental (HPLC-UV-mass spectrometry and infrared spectroscopy) and computational (density functional theory) studies. Against all odds, the EGCG–sucrose complex under certain conditions may have prevented EGCG from degradation in aqueous media. Indeed, in agreement with the ICH guidelines, the formulated solution was shown to be stable up to at least 24 months under 2–8 °C and at ambient temperature. Furthermore, considerable improvement in bioavailability in rats, against EGCG powder formulated in hard-gel capsules, was shown after gavage. Thus, the proposed formulation may provide an easily implementable platform to administer EGCG in the context of clinical development.https://www.mdpi.com/1424-8247/14/12/1242epigallocatechin gallateformulationcomplexstabilitymass spectrometrydensity functional theory |
| spellingShingle | Philippe-Henri Secretan Olivier Thirion Hassane Sadou Yayé Thibaud Damy Alain Astier Muriel Paul Bernard Do Simple Approach to Enhance Green Tea Epigallocatechin Gallate Stability in Aqueous Solutions and Bioavailability: Experimental and Theoretical Characterizations Pharmaceuticals epigallocatechin gallate formulation complex stability mass spectrometry density functional theory |
| title | Simple Approach to Enhance Green Tea Epigallocatechin Gallate Stability in Aqueous Solutions and Bioavailability: Experimental and Theoretical Characterizations |
| title_full | Simple Approach to Enhance Green Tea Epigallocatechin Gallate Stability in Aqueous Solutions and Bioavailability: Experimental and Theoretical Characterizations |
| title_fullStr | Simple Approach to Enhance Green Tea Epigallocatechin Gallate Stability in Aqueous Solutions and Bioavailability: Experimental and Theoretical Characterizations |
| title_full_unstemmed | Simple Approach to Enhance Green Tea Epigallocatechin Gallate Stability in Aqueous Solutions and Bioavailability: Experimental and Theoretical Characterizations |
| title_short | Simple Approach to Enhance Green Tea Epigallocatechin Gallate Stability in Aqueous Solutions and Bioavailability: Experimental and Theoretical Characterizations |
| title_sort | simple approach to enhance green tea epigallocatechin gallate stability in aqueous solutions and bioavailability experimental and theoretical characterizations |
| topic | epigallocatechin gallate formulation complex stability mass spectrometry density functional theory |
| url | https://www.mdpi.com/1424-8247/14/12/1242 |
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