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Antioxidants
Volume 12
Issue 2
10.3390/antiox12020424
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Article

3D-Printed, Liquid-Filled Capsules of Concentrated and Stabilized Polyphenol Epigallocatechin Gallate, Developed in a Clinical Trial

by
Philippe-Henri Secretan
1,*,
Victoire Vieillard
2,
Olivier Thirion
2,
Maxime Annereau
1,3,
Hassane Sadou Yayé
4,
Alain Astier
2,
Muriel Paul
2,5,
Thibaud Damy
6 and
Bernard Do
1,2
1
Matériaux et Santé, Université Paris-Saclay, 91400 Orsay, France
2
Department of Pharmacy, Henri Mondor Hospital, AP-HP, 94000 Créteil, France
3
Clinical Pharmacy Department, Gustave Roussy Cancer Campus, 94805 Villejuif, France
4
Department of Pharmacy, Hôpitaux Universitaires Pitié-Salpêtrière, AP-HP, 75013 Paris, France
5
EpidermE, University Paris Est Creteil, 94010 Creteil, France
6
Department of Cardiology, Henri Mondor Hospital, AP-HP, 94000 Créteil, France
*
Author to whom correspondence should be addressed.
Antioxidants 2023, 12(2), 424; https://doi.org/10.3390/antiox12020424
Submission received: 16 January 2023 / Revised: 6 February 2023 / Accepted: 7 February 2023 / Published: 9 February 2023
(This article belongs to the Special Issue Natural Antioxidants: Characterization, Synthetic Analogues and Potential Applications)
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Abstract

In vitro studies have shown that epigallocatechin gallate (EGCG), the most potent antioxidant of the green tea polyphenol catechins, is able to effectively prevent the formation of amyloid plaques and induce their clearance. However, its high chemical reactivity promotes high chemical instability, which represents a major obstacle for the development of pharmaceutical forms containing solubilized EGCG, an essential condition for a better systemic passage via the oral route. After discovering that EGCG forms a deep eutectic with choline chloride, we exploited this property to formulate and patent liquid-filled capsules containing 200–800 mg of soluble EGCG in easy-to-administer sizes. The gelatin envelopes used are of the conventional type and their filling has been achieved using 3D printing technology. Not only did the EGCG-choline complex allow the formulation of hydrophilic solutions with a high concentration of active substance but it also contributed significantly to its chemical stability, since after at least 18 months of storage at 25 °C/60% RH and one year at 40 °C/75% RH, the capsules show unchanged hardness, chromatographic profiles and antioxidant activity compared to T0. Preclinical studies in monkeys showed that bioavailability was increased by a factor of 10 compared to marketed capsules comprising EGCG powder. This pharmaceutical development was conducted in the context of upcoming clinical trials to evaluate EGCG alone or in combination when treating transthyretin and light-chain cardiac amyloidosis.
Keywords: epigallocatechin gallate; formulation; eutectic solution; stability; bioavailability; oral solution epigallocatechin gallate; formulation; eutectic solution; stability; bioavailability; oral solution

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MDPI and ACS Style

Secretan, P.-H.; Vieillard, V.; Thirion, O.; Annereau, M.; Yayé, H.S.; Astier, A.; Paul, M.; Damy, T.; Do, B. 3D-Printed, Liquid-Filled Capsules of Concentrated and Stabilized Polyphenol Epigallocatechin Gallate, Developed in a Clinical Trial. Antioxidants 2023, 12, 424. https://doi.org/10.3390/antiox12020424

AMA Style

Secretan P-H, Vieillard V, Thirion O, Annereau M, Yayé HS, Astier A, Paul M, Damy T, Do B. 3D-Printed, Liquid-Filled Capsules of Concentrated and Stabilized Polyphenol Epigallocatechin Gallate, Developed in a Clinical Trial. Antioxidants. 2023; 12(2):424. https://doi.org/10.3390/antiox12020424

Chicago/Turabian Style

Secretan, Philippe-Henri, Victoire Vieillard, Olivier Thirion, Maxime Annereau, Hassane Sadou Yayé, Alain Astier, Muriel Paul, Thibaud Damy, and Bernard Do. 2023. "3D-Printed, Liquid-Filled Capsules of Concentrated and Stabilized Polyphenol Epigallocatechin Gallate, Developed in a Clinical Trial" Antioxidants 12, no. 2: 424. https://doi.org/10.3390/antiox12020424

APA Style

Secretan, P.-H., Vieillard, V., Thirion, O., Annereau, M., Yayé, H. S., Astier, A., Paul, M., Damy, T., & Do, B. (2023). 3D-Printed, Liquid-Filled Capsules of Concentrated and Stabilized Polyphenol Epigallocatechin Gallate, Developed in a Clinical Trial. Antioxidants, 12(2), 424. https://doi.org/10.3390/antiox12020424

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