Marine phospholipid nanoliposomes: A promising therapeutic approach for inflammatory bowel disease: Preparation, safety, and efficacy evaluation.

ABSTRACT

Promising findings have been emerged from studies utilizing n3 polyunsaturated fatty acids (PUFA) supplementation in animal models of inflammatory bowel disease (IBD). Introduction of marine phospholipids which combine n3 PUFA with phosphatidylcholine in a nanoliposome formulation offers enhanced pharmacological efficacy due to physical stability, improved bioavailability, and specific targeting to inflamed colitis tissues. In the present study, a marine phospholipid-based nanoliposome formulation was developed and optimized, resulting in nanovesicles of approximately 107.7 ± 1.3 nm in size, 0.18 ± 0.01 PDI, and - 32.03 ± 3.16 mV ZP. The nanoliposomes exhibited spherical vesicles with stable properties upon incubation at SGF as shown by the TEM, DLS, and turbidity measurements over 3 h. MPL nanoliposomes were cytocompatible until the concentration of 500 µg/mL as per MTT assay and taken by macrophages through macropinocytosis and caveolae pathways, and demonstrated significant inhibitory activity against reactive oxygen species (ROS) in LPS-stimulated macrophages. They were also shown to be blood-compatible and safe for administration in healthy mice. In a colitis mouse model, the nanoliposomes displayed preferential distribution in the inflamed gut, delaying the onset of colitis when administered prophylactically. These findings highlight the potential of marine phospholipid nanoliposomes as a promising therapeutic approach for managing inflammatory bowel disease.