Functional Role of VCAM-1 Targeted Flavonoid-Loaded Lipid Nanoemulsions in Reducing Endothelium Inflammation.

摘要: Citrus flavonoids have well-documented protective effects on cardiovascular system, but the poor water solubility and reduced bioavailability restrict their therapeutic use. We aimed to overcome these limitations encapsulated naringenin hesperetin into lipid nanoemulsions (LNs), targeted vascular cell adhesion molecule-1 (VCAM-1), which is expressed activated endothelial cells (ECs). LNs were characterized by a hydrodynamic size of ~200 nm, negative zeta potential, an encapsulation efficiency higher than 80%, good in vitro stability steady release cargo. The neither cytotoxic human ECs line EA.hy926, nor provoked lysis murine erithrocytes. Then, we tested whether nanoformulations reduce tumor necrosis factor-alpha (TNF-α) induced EC-activation. found that flavonoid-loaded LNs, either non-targeted or endothelium, taken up EA.hy926 dose-dependent manner, dependent TNF-α only case endothelium-targeted LNs. Moreover, nanoparticles inhibited both transmigration THP-1 monocytes on/through ECs, mechanisms involving expression pro-inflammatory chemokine monocyte chemotactic protein 1 (MCP-1) diminished nuclear translocation factor kappa-light-chain-enhancer B (NF-κB).