Work

Preparation of colon-targeted pellets loaded with filgotinib/berberine hydrochloride and Their application in ulcerative colitis therapy

Year: 2025

Type: article

Abstract: Ulcerative colitis (UC) is a recurrent-remitting autoimmune disease of the colon, the pathogenesis of which remains incompletely understood. Recent studies have revealed gut dysbiosis and immune imbalance mediated by the JAK-STAT and NF-κB signaling pathways are closely associated with the onset and progression of UC. In particular, the interplay between gut dysbiosis and immune imbalance has become a key factor in the rapid progression of UC, which also contributes to the suboptimal efficacy of existing therapeutic drugs. A growing number of scholars believe that simultaneously regulating gut dysbiosis and immune imbalance to synergistically combat UC may represent a critical breakthrough in UC treatment. Based on this premise, this study utilized extrusion-spheronization and fluidized-bed-coating technologies to prepare colon-targeted pellets co-loaded with berberine hydrochloride and filgotinib, and evaluated their potential for synergistic UC therapy. The results demonstrated the prepared pellets exhibited satisfactory pharmaceutical characteristics, including high sphericity, uniform particle size, and intact coating integrity. Moreover, the drug release behavior of the pellets showed high consistency in both in-vitro and in-vivo settings, displaying distinct pH-responsive release properties that meet the requirements for colon-targeted formulations. Furthermore, the pellets exhibited significant therapeutic effects in DSS-induced UC model, with beneficial changes observed in key indicators such as gut microbiota and immune. Immunohistochemistry, multiplex cytokine assays, and gut microbiota sequencing results all confirmed the synergistic effect of berberine hydrochloride and filgotinib in UC treatment. In conclusion, the findings of this study provide new insights for further research on UC and the development of synergistic UC therapies.

Source: International Journal of Pharmaceutics X

DOI: 10.1016/j.ijpx.2025.100415

Authors: Jinglong Wang, Zhixuan Kuang, Binglian Chen, Chenxi Yan, Bowen Shi, Guofei Li

Institutions: Sheng Jing Hospital, Aerospace Center Hospital, China Medical University

Language: English

Topic: Advanced Drug Delivery Systems

Subfield: Pharmaceutical Science

Field: Pharmacology, Toxicology and Pharmaceutics

Domain: Life Sciences

SDG: Good health and well-being

Open Access status: gold

Estimated APC paid: $2,590