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).

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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

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article

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

Zhe Chi, Hamed I. Hamouda, Samah Shabana, Chenguang Liu et al.
2 citations
Journal of Drug Delivery Science and Technology
Infant Nutrition and Health
2.24
article

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

Zhe Chi, Hamed I. Hamouda, Samah Shabana, Chenguang Liu, Suzan Noureldin
article en
2 citations

Abstract

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).

Journal of Drug Delivery Science and TechnologyVol. 108
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)
Chinese Academy of Sciences, China Scholarship Council, Natural Science Foundation of Shandong Province, Dalian Institute of Chemical Physics
Life below water
Openalex Percentile: Top 15%
Infant Nutrition and Health
2.24
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