Next Article in Journal
Pharmacokinetic Profile and Anti-Adhesive Effect of Oxaliplatin-PLGA Microparticle-Loaded Hydrogels in Rats for Colorectal Cancer Treatment
Previous Article in Journal
Application of Micro-Scale 3D Printing in Pharmaceutics
Open AccessArticle

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

1
Institute of Cellular Biology and Pathology “Nicolae Simionescu”, 050568 Bucharest, Romania
2
Faculty of Biotechnologies, University of Agronomic Sciences and Veterinary Medicine (UASVM), 011464 Bucharest, Romania
3
Faculty of Veterinary Medicine, University of Agronomic Sciences and Veterinary Medicine (UASVM), 050097 Bucharest, Romania
*
Author to whom correspondence should be addressed.
Pharmaceutics 2019, 11(8), 391; https://doi.org/10.3390/pharmaceutics11080391 (registering DOI)
Received: 2 July 2019 / Revised: 26 July 2019 / Accepted: 1 August 2019 / Published: 3 August 2019
(This article belongs to the Special Issue Emergent Strategies for Natural Products Delivery)
  |  
PDF [5192 KB, uploaded 22 August 2019]
  |  

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 monocyte chemotactic protein 1 (MCP-1) and diminished nuclear translocation of nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB). View Full-Text
Keywords: cell-targeting peptide; naringenin; hesperetin; endothelium; lipid nanoemulsions; nanoparticle cell-targeting peptide; naringenin; hesperetin; endothelium; lipid nanoemulsions; nanoparticle
Figures

Graphical abstract

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

Share & Cite This Article

MDPI and ACS Style

Fuior, E.V.; Deleanu, M.; Constantinescu, C.A.; Rebleanu, D.; Voicu, G.; Simionescu, M.; Calin, M. Functional Role of VCAM-1 Targeted Flavonoid-Loaded Lipid Nanoemulsions in Reducing Endothelium Inflammation. Pharmaceutics 2019, 11, 391.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Pharmaceutics EISSN 1999-4923 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top