The pathogenesis of inflammatory bowel diseases (IBDs)
including
ulcerative colitis (UC) and Crohn’s disease is extremely cloudy.
Maintaining the level of remission lesions in colitis is the default
treatment attitude at present. Epithelial barrier restoration is considered
as the same important strategy as colonic targeted drug delivery in
UC treatment. In this paper, we developed a multilayer natural polysaccharide
microsphere (pectin/chitosan/alginate) with pH and enzyme dual sensitivity
to reduce the loss of medication in the upper digestive tract and
preferentially adhere to exposed epithelial cells in colonic tissues
by electrostatic forces for efficiently targeted UC treatment. Olsalazine
as an inflammatory drug was efficiently loaded in the chitosan layer
and realized a colonic pH-responsive drug release. Furthermore, the
multilayer microspheres exhibited excellent capability in suppressing
harmful flora and a bio-adhesion effect to extend the duration of
local medicine. In the in vivo anti-colitis study, the downregulated
levels of pro-inflammatory factors and the increase of tight junction
protein indicated the excellent anti-inflammation effect of the olsalazine-loaded
microspheres. In summary, these results showed that the multilayer
natural polysaccharide microspheres could be a powerful candidate
in the targeted drug delivery system for UC therapy.