Rapid-release and user-friendly costunolide/dehydrocostuslactone hydrophilic nanofibers: Therapeutic effects on acute gastric ulcers

Gastric ulcers often cause postprandial epigastric pain, especially in acute cases. Abnormal motility, with about 50 % of patients having delayed gastric emptying, contributes to ulcer development. Costunolide (COS) and dehydrocostuslactone (DEH), derived from "Mu xiang" herbs, show potential in treating ulcers and regulating gastrointestinal motility. However, their poor solubility and bioavailability limit in vivo use. This study uses electrospinning to develop hydrophilic nanofibers loaded with COS and DEH in a polyvinylpyrrolidone (PVP) matrix for treating acute gastric ulcers. The production process for costunolide / dehydrocostuslactone nanofibers (COS/DEH/NFs) was optimized, characterized, and tested in pharmacodynamic studies. The results showed that COS and DEH remained in a non-crystalline state within COS/DEH/NFs, enhancing their in vitro release. With 21 % drug incorporation, COS/DEH/NFs released over 70 % of COS and more than 50 % of DEH within 20 min in body fluids. In treatment, COS/DEH/NFs suppressed pro-inflammatory cytokines, resisted oxidative stress, promoted gastric mucosal repair, and enhanced gastrointestinal motility. In a mouse model of acute gastric ulcer, high-dose COS/DEH/NFs achieved a 77.09 % ulcer inhibition rate, and low-dose COS/DEH/NFs resulted in gastric residual and intestinal propulsion rates of 73.55 % and 69.89 %, respectively. The drug loading of COS/DEH/NFs is 14.76 ± 0.26 %, with an encapsulation efficiency of 68.77 ± 1.14 %. COS/DEH/NFs is a new choice for treating acute gastric ulcers with gastrointestinal bloating due to its convenience and swallow-free use, providing rapid symptom relief.