Year-end Sale % OFF 
Abstract
Epigallocatechin gallate (EGCG) has been recognized as the most prominent green tea extract due to its healthy influences. The high instability and low bioavailability, however, strongly limit its utilization in food and drug industries. This work, for the first time, develops amorphous solid dispersion of EGCG to enhance its bioavailability and physical stability. Four commonly used polymeric excipients are found to be compatible with EGCG in water-dioxane mixtures via a stepwise mixing method aided by vigorous mechanical interference. The dispersions are successfully generated by lyophilization. The physical stability of the dispersions is significantly improved compared to pure amorphous EGCG in stress condition (elevated temperature and relative humidity) and simulated gastrointestinal tract environment. From the drug release tests, one of the dispersions, EGCG-Soluplus® 50:50 (w/w) shows a dissolution profile that only 50% EGCG is released in the first 20 min, and the remains are slowly released in 24 h. This sustained release profile may open up new possibilities to increase EGCG bioavailability via extending its elimination time in plasma.
Highlights
Green tea has been one of the most popular and consumed beverages, widely recognized for its healthy influences, since ancient times [1]
Nine polymers that are commonly used as pharmaceutical excipients were initially screened for their solubility, compatibility with epigallocatechin gallate (EGCG) in solvents, and crystallinity after lyophilization
Precipitates were observed in the mixtures containing EGCG with polyvinylpyrrolidone (PVP K-90), polyvinyl alcohol (PVA), polyethylene glycol (PEG), and polyvinyl acetate (PVAc), and these samples did not move forward with dispersion preparation
Summary
Green tea has been one of the most popular and consumed beverages, widely recognized for its healthy influences, since ancient times [1]. A more commonly hypothesized approach to improve the bioavailability is to decrease the dissolution rate and solubility, and establish a sustained release of EGCG in the GI tract. Methods such as encapsulation or making insoluble complex [33,40] result in a slower release of EGCG from the capsulated structure/complex, which diminishes its chemical degradation in the GI tract. The approach of amorphous solid dispersion is employed targeting the enhancement of the bioavailability and physical stability of EGCG. This work employs a convenient lyophilization approach to generate EGCG amorphous solid dispersions targeting two objectives: (1) improve physical stability of EGCG in common storage/processing and simulated GI environments; (2) establish a sustained release that may potentially enhance oral bioavailability. To the best knowledge of the authors, this is the first work generating EGCG amorphous solid dispersions aiming at minimize these two critical issues
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
