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. 2017 Nov 9;10(4):88.
doi: 10.3390/ph10040088.

Amorphous Solid Dispersion of Epigallocatechin Gallate for Enhanced Physical Stability and Controlled Release

Yizheng Cao  1 , Jing Teng  2 , Jon Selbo  3
Affiliations

Amorphous Solid Dispersion of Epigallocatechin Gallate for Enhanced Physical Stability and Controlled Release

Yizheng Cao et al. Pharmaceuticals (Basel). .

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.

Keywords: amorphous solid dispersion; bioavailability; controlled release; epigallocatechin gallate; physical stability.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Hierarchical terminology of green tea extracts down to epigallocatechin gallate (EGCG).
Figure 2
Figure 2
Chemical structure of EGCG.
Figure 3
Figure 3
The XRPD patterns of the four dispersions, aEGCG, and cEGCG.
Figure 4
Figure 4
SEM images of (a,b) cEGCG; (c,d) aEGCG; and dispersions of EGCG with (e,f) HPMCAS; (g,h) HPMCP; (i,j) Soluplus®; and (k,l) cellulose acetate.
Figure 4
Figure 4
SEM images of (a,b) cEGCG; (c,d) aEGCG; and dispersions of EGCG with (e,f) HPMCAS; (g,h) HPMCP; (i,j) Soluplus®; and (k,l) cellulose acetate.
Figure 5
Figure 5
TGA results of the four dispersions, aEGCG and cEGCG.
Figure 6
Figure 6
mDSC results of the four dispersions and aEGCG.
Figure 7
Figure 7
XRPD patterns of the dispersions and aEGCG after stressed at 40 °C/75% RH for 11 days.
Figure 8
Figure 8
The XRPD patterns of the post-dissolution solids from EGCG-Soluplus® and EGCG-cellulose acetate dispersions.
Figure 9
Figure 9
EGCG release profiles for cEGCG, aEGCG, and the dispersions in pH 7.4 PBS medium at 37 °C.
Figure 10
Figure 10
Comparison of EGCG release from the cEGCG, aEGCG, and the dispersions in the first 20 min in pH 7.4 PBS medium at 37 °C.
Figure 11
Figure 11
The pseudo second-order fitting for (a) cEGCG; (b) aEGCG; (c) EGCG-HPMCAS; (d) EGCG-HPMCP; (e) EGCG-cellulose acetate; and (f) EGCG-Soluplus®.
Figure 12
Figure 12
The release profile of Soluplus®-EGCG dispersion fitted with biphasic PSO-FO model.
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