The application is a colon-targeting lipid
nanoparticle based on
ginsenoside Rg3, a
calcium alginate
microsphere thereof and application thereof in treating
ulcerative colitis, and belongs to the technical field of new excipients and new dosage forms of pharmaceutical preparations, and particularly relates to an oral colon-targeting
delivery system for treating
ulcerative colitis. The
system replaces
cholesterol in traditional lipid nanoparticles with
ginsenoside Rg3, constructs lipid nanoparticles capable of efficiently loading TNF-alpha siRNA, and effectively improves the targeting property and
lysosome escape ability of the lipid nanoparticles on inflammatory macrophages. In order to further realize colon-specific delivery, the above-mentioned lipid nanoparticles are loaded in a pH-responsive
calcium alginate
microsphere, so that the
drug is kept stable in the
upper gastrointestinal tract and is released in a responsive manner in the colon. Pharmacodynamic studies show that the
drug delivery system can significantly relieve the symptoms of
colitis, effectively
silence the expression of TNF-alpha, repair the intestinal barrier, and regulate the intestinal microbiota. The application provides a safe and efficient new strategy for solving the problems of poor gastrointestinal stability and low targeting efficiency of oral delivery of
nucleic acid drugs.