Marine phospholipid nanoliposomes mediate oral colonic delivery of 5-aminosalicylic acid and mitigate the severity of DSS-induced colitis in mouse models
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. • Marine phospholipid nanoliposomes were effective in hydrophilic drug encapsulation. • MPL nanoliposomes demonstrated a synergistic effect, enhancing drug efficacy and therapeutic outcomes. • Marine phospholipid nanoliposomes offer breakthrough potential for drug delivery in inflammatory bowel disease (IBD).
Authors
- Zhe Chi (ORCID: https://orcid.org/0000-0002-8794-1940)
- Hamed I. Hamouda (ORCID: https://orcid.org/0000-0002-5980-0796)
- Samah Shabana (ORCID: https://orcid.org/0000-0001-5624-8089)
- Chenguang Liu (ORCID: https://orcid.org/0000-0002-9995-4853)
- Suzan Noureldin
Institutions
- Dalian Institute of Chemical Physics (CN)
- Chinese Academy of Sciences (CN)
- Dalian University of Technology (CN)
- Dalian University (CN)
- Jiangsu University of Science and Technology (CN)
- Jiangsu University of Technology (CN)
- Ministry of Health and Population (EG)
- Ocean University of China (CN)
- Egyptian Petroleum Research Institute (EG)
Publication Details
- Journal
- Journal of Drug Delivery Science and Technology
- Published
- 2025-03-27
- DOI
- https://doi.org/10.1016/j.jddst.2025.106821
- Citations
- 2
- Primary Topic
- Infant Nutrition and Health
- Type
- article
- Field-Weighted Citation Impact
- 2.24
Funders
- Chinese Academy of Sciences
- China Scholarship Council
- Natural Science Foundation of Shandong Province
- Dalian Institute of Chemical Physics