Macrophage-Targeted Berberine-Loaded β-Glucan Nanoparticles Enhance the Treatment of Ulcerative Colitis

• Published in: International journal of nanomedicine Vol. 17; pp. 5303 - 5314
• Main Authors: Xu, Yuying, Huang, Jintao, Fan, Yapei, Long, Haiyue, Liang, Minting, Chen, Qunjie, Wang, Zhiping, Wu, Chaoxi, Wang, Yifei
• Format: Journal Article
• Language: English
• Published: New Zealand Taylor & Francis Ltd 01.01.2022; Dove; Dove Medical Press
• Subjects: Animals; anti-inflammation; Anti-Inflammatory Agents - pharmacology; Anti-Inflammatory Agents - therapeutic use; Berberine - pharmacology; Berberine - therapeutic use; beta-Glucans; Cell culture; chiral; Colitis - chemically induced; Colitis, Ulcerative - chemically induced; Colitis, Ulcerative - drug therapy; Cytokines; drug carrier; Drug delivery systems; Drugs; Hemodialysis; immunoregulation; Inflammation - drug therapy; Inflammatory bowel disease; Interleukin-6; Laboratory animals; Lipopolysaccharides; Macrophages; Mice; Mice, Inbred C57BL; Microscopy; Nanoparticles; Original Research; Solvents; Spectrum analysis; Yeast; β-glucan; United Kingdom > UK; United States > US; China; β-glucan; immunoregulation; anti-inflammation; chiral; drug carrier
• ISSN: 1178-2013; 1176-9114; 1178-2013
• DOI: 10.2147/IJN.S379792

This study focuses on constructing of an anti-inflammatory drug delivery system by encapsulation of berberine in the β-glucan nanoparticles and evaluates its effect on treating ulcerative colitis. β-Glucan and the anti-inflammatory drug berberine (BER) are self-assembled into nanoparticles to construct a drug delivery system (GLC/BER). The interaction between the drug and the carrier was characterized by circular dichroism, ultraviolet-visible spectroscopy, and dynamic light scattering. The anti-inflammatory effect of the GLC/BER was evaluated through a lipopolysaccharide (LPS)-induced RAW264.7 macrophage inflammation model and a sodium sulfate (DSS)-induced C57BL/6 mouse ulcerative colitis model. The GLC/BER nanoparticles have a particle size of 80-120 nm and a high encapsulation efficiency of 37.8±4.21%. In the LPS-induced RAW264.7 macrophage inflammation model, GLC/BER significantly promoted the uptake of BER by RAW264.7 cells. RT-PCR and ELISA assay showed that it could significantly inhibit the inflammatory factors including IL-1β, IL-6 and COX-2. Furthermore, GLC/BER shows inhibiting effect on the secretion of pro-inflammatory factors such as IL-1β and IL-6, down-regulating the production of nitrite oxide; in animal studies, GLC/BER was found to exert a relieving effect on mice colitis. The study found that GLC/BER has an anti-inflammatory effect in vitro and in vivo, and the GLC carrier improves the potency and bioavailability of BER, providing a new type of nanomedicine for the treatment of colitis.