Starch nanoparticle platform for oral delivery of sinigrin in colitis therapy

Abstract

Sinigrin, a glucosinolate known for its potential therapeutic effects on ulcerative colitis (UC), suffers from rapid gastric clearance and low bioavailability when administered orally. To address these limitations, we developed a novel delivery system using starch nanoparticles (SNPs) to encapsulate sinigrin via a sinigrin-lecithin complex (SNG-L). This approach significantly improved sinigrin's encapsulation efficiency, stability against acidic degradation, and controlled release in simulated intestinal conditions. In vivo studies using a preclinical UC mouse model demonstrated that SNG-L@SNPs effectively targeted and released sinigrin into the intestine, where it was converted into the bioactive compound allyl isothiocyanate (AITC) through the intestinal microflora. This targeted delivery and controlled release system markedly alleviated the pathological manifestations of UC and preserved intestinal barrier integrity by mitigating tight junction disruption and apoptosis of intestinal epithelial cells (IECs) through reduction of oxidative stress. These findings highlight the potential of this precise and sustained drug delivery system as an effective therapeutic strategy for UC management.