Marine phospholipid nanoliposomes mediate oral colonic delivery of 5-aminosalicylic acid and mitigate the severity of DSS-induced colitis in mouse models

结肠炎 氨基水杨酸 磷脂 脂质体 溃疡性结肠炎 医学 化学 胃肠病学 内科学 生物化学 疾病
作者
Samah Shabana,Hamed I. Hamouda,Suzan Noureldin,Zhe Chi,Chenguang Liu
出处
期刊:Journal of Drug Delivery Science and Technology [Elsevier BV]
卷期号:108: 106821-106821 被引量:2
标识
DOI:10.1016/j.jddst.2025.106821
摘要

5-Aminosalicylic acid (5-ASA) is the preferred medication for treating mild to moderate inflammatory bowel disease (IBD). However, side effects and sometimes insufficient efficacy pose challenges. This study introduces chitosan-coated orally targeted marine phospholipid nanoliposomes grafted with Vit. E. TPGS for delivering 5-aminosalicylic acid to the inflamed mucosa in IBD treatment. MTL nanoliposomes were prepared by the thin film hydration method, exhibiting sizes of 165.8 ± 2.19 nm pre-coating and 259.5 ± 1.77 nm size post-coating. The nanoliposomes showed controlled drug release at intestinal pH, with minimal release in the simulated gastric medium. They demonstrated excellent stability over a 45-day storage period. In vitro , cytocompatibility studies with L929 cells and ex vivo studies with RBCs showed excellent biocompatibility . MTL nanoliposomes showed selective deposition in inflamed RAW 264.7 macrophages and time-dependent uptake in Caco2 intestinal cells. In vitro, anti-inflammatory experiments significantly reduced inflammatory biomarkers like TNF-α, IL1-β, IL-6, and ROS. In vivo, DSS-induced colitis studies demonstrated improved colitis indices, colonic tissue change restoration, and myeloperoxidase activity inhibition. These findings underscore the potential of MTL nanoliposomes as a promising targeted delivery system for 5-aminosalicylic acid in treating IBD.
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