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

Int J Nanomedicine. 2022 Nov 14:17:5303-5314. doi: 10.2147/IJN.S379792. eCollection 2022.

Abstract

Aim: 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.

Methods: 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.

Results: 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.

Conclusion: 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.

Keywords: anti-inflammation; chiral; drug carrier; immunoregulation; β-glucan.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / pharmacology
  • Anti-Inflammatory Agents / therapeutic use
  • Berberine* / pharmacology
  • Berberine* / therapeutic use
  • Colitis* / chemically induced
  • Colitis, Ulcerative* / chemically induced
  • Colitis, Ulcerative* / drug therapy
  • Inflammation / drug therapy
  • Interleukin-6
  • Lipopolysaccharides
  • Macrophages
  • Mice
  • Mice, Inbred C57BL
  • Nanoparticles*
  • beta-Glucans*

Substances

  • Berberine
  • beta-Glucans
  • Lipopolysaccharides
  • Interleukin-6
  • Anti-Inflammatory Agents