Exploiting marine phospholipid nanoliposomes for enhanced apremilast delivery and therapeutic efficacy in inflammatory bowel disease

Marine phospholipid (MPL) nanoliposomes represent a new frontier in drug delivery systems , offering unique bio-functional and physicochemical properties. This study developed orally administered MPL nanoliposomes to enhance apremilast delivery and bioavailability in inflamed bowel disease (IBD). Drug release studies showed effective gastric protection (21.2 ± 0.4 % release at pH 1.2 after 2 h) and substantial release (96.4 ± 0.3 %) at pH 6.8 over 12 h. The optimized formulation (4 % drug w/w) showed remarkable stability over 6 weeks of storage at 4 °C. Apr/MPL nanoliposomes up to 300 µg/mL showed great cytocompatibility to RAW 264.7 macrophages and Caco2 intestinal cells. Furthermore, the formulation exhibited superior anti-inflammatory effects, significantly reducing nitric oxide (NO) production and downregulating pro-inflammatory cytokines (TNF-α, IL-1β, IL-6) in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages. In vivo , Apr/MPL nanoliposomes improved recovery in a dextran sulfate sodium (DSS)-induced ulcerative colitis model, outperforming free apremilast. These findings underscore MPL nanoliposomes as a promising pharmacological tool for managing inflammation and a versatile drug delivery system for IBD. Scheme: Schematic representation of Apr/MPL nanoliposome development by thin film hydration procedure and its potential in treating dextran sulfate sodium (DSS)-induced colitis. • Marine phospholipid nanoliposomes enable apremilast oral delivery to inflamed bowel. • The nanoliposome demonstrated excellent drug protection and stability during storage. • Apremilast nanoliposome: potent anti-inflammatory in vitro in inflamed macrophages. • Apremilast nanoliposome: improved ulcerative colitis model compared to apremilast.