Study on the preparation of EGCG-γ-Cyclodextrin inclusion complex and its drug-excipient combined therapeutic effects on the treatment of DSS-induced acute ulcerative colitis in mice

• Published in: International journal of pharmaceutics Vol. 630; p. 122419
• Main Authors: Wang, Weiqin, Li, Xuefeng, Shi, Fanli, Zhang, Zhenhai, Lv, Huixia
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 05-01-2023
• Subjects: Anti-inflammatory; Cyclodextrin; EGCG; Inclusion complex; Intestinal flora; Ulcerative colitis; Cyclodextrin; Intestinal flora; Anti-inflammatory; EGCG; Inclusion complex; Ulcerative colitis
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2022.122419

[Display omitted]
In this study, γ-cyclodextrins (γ-CD) and epigallocatechin-3-gallate (EGCG) were designed to form an inclusion complex (EGCG-γ-IC) for ulcerative colitis (UC) treatment. The drug-excipient combined therapeutic potential of γ-CD and EGCG was verified, when stability and compliance were also achieved. EGCG-γ-IC effectively inhibited the secretions of NO, TNF-α, and IL-6 and the intracellular ROS in RAW264.7 cells. The effectiveness of EGCG-γ-IC in treating DSS-induced acute UC in mice was observed including improving the histological conditions of the colon, reducing the levels of IL-1β, IL-6, and TNF-α in serum, and restoring MPO, GSH, and sIgA levels in intestinal tissues. Moreover, EGCG-γ-IC had a more prominent effect on regulating bacterial dysbiosis caused by DSS than EGCG and γ-CD alone. Therefore, EGCG-γ-IC designed here displayed UC treating capacity with safety in the long-term application and promised an industrial production potential due to its excellent storage stability.