PMID- 31382634
OWN - NLM
STAT- PubMed-not-MEDLINE
LR  - 20231013
IS  - 1999-4923 (Print)
IS  - 1999-4923 (Electronic)
IS  - 1999-4923 (Linking)
VI  - 11
IP  - 8
DP  - 2019 Aug 3
TI  - Functional Role of VCAM-1 Targeted Flavonoid-Loaded Lipid Nanoemulsions in 
      Reducing Endothelium Inflammation.
LID - 10.3390/pharmaceutics11080391 [doi]
LID - 391
AB  - 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-alpha) 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-alpha 
      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-kappaB).
FAU - Fuior, Elena Valeria
AU  - Fuior EV
AD  - Institute of Cellular Biology and Pathology "Nicolae Simionescu", 050568 
      Bucharest, Romania.
FAU - Deleanu, Mariana
AU  - Deleanu M
AD  - Institute of Cellular Biology and Pathology "Nicolae Simionescu", 050568 
      Bucharest, Romania.
AD  - Faculty of Biotechnologies, University of Agronomic Sciences and Veterinary 
      Medicine (UASVM), 011464 Bucharest, Romania.
FAU - Constantinescu, Cristina Ana
AU  - Constantinescu CA
AD  - Institute of Cellular Biology and Pathology "Nicolae Simionescu", 050568 
      Bucharest, Romania.
AD  - Faculty of Veterinary Medicine, University of Agronomic Sciences and Veterinary 
      Medicine (UASVM), 050097 Bucharest, Romania.
FAU - Rebleanu, Daniela
AU  - Rebleanu D
AD  - Institute of Cellular Biology and Pathology "Nicolae Simionescu", 050568 
      Bucharest, Romania.
FAU - Voicu, Geanina
AU  - Voicu G
AD  - Institute of Cellular Biology and Pathology "Nicolae Simionescu", 050568 
      Bucharest, Romania.
FAU - Simionescu, Maya
AU  - Simionescu M
AD  - Institute of Cellular Biology and Pathology "Nicolae Simionescu", 050568 
      Bucharest, Romania.
FAU - Calin, Manuela
AU  - Calin M
AUID- ORCID: 0000-0002-5245-160X
AD  - Institute of Cellular Biology and Pathology "Nicolae Simionescu", 050568 
      Bucharest, Romania. manuela.calin@icbp.ro.
LA  - eng
GR  - 13PCCDI/2018/Unitatea Executiva pentru Finantarea Invatamantului Superior, a 
      Cercetarii, Dezvoltarii si Inovarii/
GR  - CARDIOPRO Project ID: 143/ERDF co-financed investment in RTDI for 
      Competitiveness/
PT  - Journal Article
DEP - 20190803
PL  - Switzerland
TA  - Pharmaceutics
JT  - Pharmaceutics
JID - 101534003
PMC - PMC6722676
OTO - NOTNLM
OT  - cell-targeting peptide
OT  - endothelium
OT  - hesperetin
OT  - lipid nanoemulsions
OT  - nanoparticle
OT  - naringenin
COIS- The authors declare no conflict of interest regarding the publication of this 
      paper.
EDAT- 2019/08/07 06:00
MHDA- 2019/08/07 06:01
PMCR- 2019/08/01
CRDT- 2019/08/07 06:00
PHST- 2019/06/30 00:00 [received]
PHST- 2019/07/26 00:00 [revised]
PHST- 2019/08/01 00:00 [accepted]
PHST- 2019/08/07 06:00 [entrez]
PHST- 2019/08/07 06:00 [pubmed]
PHST- 2019/08/07 06:01 [medline]
PHST- 2019/08/01 00:00 [pmc-release]
AID - pharmaceutics11080391 [pii]
AID - pharmaceutics-11-00391 [pii]
AID - 10.3390/pharmaceutics11080391 [doi]
PST - epublish
SO  - Pharmaceutics. 2019 Aug 3;11(8):391. doi: 10.3390/pharmaceutics11080391.