β-1,3-D-Glucan based yeast cell wall system loaded emodin with dual-targeting layers for ulcerative colitis treatment

Herein, a beta-1,3-D-glucan based microcarrier, yeast cell wall microparticles (YPs), was used to develop a foodsource-based nano-in-micro oral delivery system for ulcerative colitis (UC) treatment. Briefly, lactoferrin (Lf), which targets intestinal epithelial cells, was used to encapsulate emodin (EMO) to form nanoparticles (EMONPs), and then loaded into YPs with the natural macrophages targeting ability, forming a final formula with two outer-inner targeting layers (EMO-NYPs). These dual-targeting strategy could enhance the dual-effects of EMO in anti-inflammatory and mucosal repair effects respectively. As expected, cell uptake assessment confirmed that EMO-NPs and EMO-NYPs could target on the Lf and dection-1 receptors on the membranes of Caco-2 cells and macrophages, respectively. Importantly, EMO-NYPs showed the best anti-UC effects compared to EMO-NPs and free EMO, by inhibiting NF-KB pathway to anti-inflammation and promoting intestinal mucosa repair via MLCK/ pMLC2 pathway. The results show that EMO-NYPs are a promising food-based oral delivery system in anti-UC.

Automated summary

This study developed a foodsource-based nano-in-micro oral delivery system for ulcerative colitis (UC) treatment using yeast cell wall microparticles. By encapsulating emodin into lactoferrin nanoparticles and loading them into yeast cell wall microparticles, a dual-targeting strategy was applied to enhance the anti-inflammatory and mucosal repair effects of emodin. Cell uptake assessment confirmed the targeting ability of the system on intestinal epithelial cells and macrophages, leading to improved anti-UC effects compared to free emodin.