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

Pharmaceutics
Elena Valeria FuiorManuela Calin

Abstract

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 and encapsulated naringenin and hesperetin into lipid nanoemulsions (LNs), targeted to vascular cell adhesion molecule-1 (VCAM-1), which is expressed on activated endothelial cells (ECs). LNs were characterized by a hydrodynamic size of ~200 nm, negative zeta potential, an encapsulation efficiency of flavonoids higher than 80%, good in vitro stability and steady release of the cargo. The LNs were neither cytotoxic to human ECs line EA.hy926, nor provoked in vitro lysis of murine erithrocytes. Then, we tested whether these nanoformulations reduce tumor necrosis factor-alpha (TNF-α) induced EC-activation. We found that flavonoid-loaded LNs, either non-targeted or targeted to the endothelium, were taken up by the EA.hy926 cells in a dose-dependent manner, but dependent on TNF-α only in the case of endothelium-targeted LNs. Moreover, these nanoparticles inhibited both the adhesion and transmigration of THP-1 monocytes on/through activated ECs, by mechanisms involving a reduced expression of the pro-inflammatory chemokine m...Continue Reading

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Citations

Dec 9, 2020·Pharmaceutics·Anna Rita BiliaMaria Camilla Bergonzi
Mar 7, 2021·Pharmaceutics·Mohammed BhiaMehdi Shakibaei
May 20, 2021·International Journal of Nanomedicine·Mahvash HesariMohammad Abdollahi

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Methods Mentioned

BETA
nuclear translocation
dynamic light scattering
electrophoretic light scattering
Assay
flow cytometry
PCR
fluorescence

Software Mentioned

Flowing
CellSens
GraphPad
Zetasizer
Agilent ChemStation
GraphPad PRISM

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