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Article

Anti-Inflammatory Effect of Cherry Extract Loaded in Polymeric Nanoparticles: Relevance of Particle Internalization in Endothelial Cells

1
Department of Life Sciences, University of Siena, via P.A. Mattioli 4, 53100 Siena, Italy
2
Cardiovascular Research Laboratory, Department of Surgery, Medical, Molecular, and Critical Area Pathology, University of Pisa, via Paradisa 2, 56100 Pisa, Italy
3
Department of Pharmacy, University of Pisa, via Bonanno 33, 56100 Pisa, Italy
4
Interdepartmental Research Center Nutraceuticals and Food for Health, University of Pisa, via Borghetto 80, 56100 Pisa, Italy
5
i3S-Instituto de Investigação e Inovação em Saúde, University of Porto, Rua Alfredo Allen 208, 4200-153 Porto, Portugal
6
INEB—Instituto de Engenharia Biomédica, Universidade do Porto, Rua Alfredo Allen, 208, 4200-135 Porto, Portugal
7
ICBAS—Instituto de Ciências Biomédicas Abel Salazar, University of Porto, Rua de Jorge Viterbo Ferreira 228, 4050-313 Porto, Portugal
8
CESPU, Instituto de Investigação e Formação Avançada em Ciências e Tecnologias da Saúde, Rua Central de Gandra, 1317, 4585-116 Gandra, Portugal
*
Authors to whom correspondence should be addressed.
Pharmaceutics 2019, 11(10), 500; https://doi.org/10.3390/pharmaceutics11100500
Received: 19 August 2019 / Revised: 18 September 2019 / Accepted: 26 September 2019 / Published: 29 September 2019
(This article belongs to the Special Issue Emergent Strategies for Natural Products Delivery)
This study aimed at evaluating the anti-inflammatory effect of natural cherry extract (CE), either free or encapsulated in nanoparticles (NPs) based on chitosan derivatives (Ch-der) or poly(lactic-co-glycolic acid) (PLGA), on human umbilical vein endothelial cells (HUVEC). CE from Prunus avium L. was characterized for total polyphenols, flavonoids, and anthocyanins content. CE and CE-loaded NP cytotoxicity and protective effect on lipopolysaccharide (LPS)-stressed HUVEC were tested by water-soluble tetrazolium salt (WST-1) assay. Pro- and anti-inflammatory cytokines (TNF-α, IL-6, IL-10, and PGE2) released by HUVEC were quantified by enzyme-linked immunosorbent assay (ELISA). All NP types were internalized into HUVEC after 2 h incubation and promoted the anti-inflammatory effect of free CE at the concentration of 2 µg gallic acid equivalents (GAE)/mL. CE-loaded Ch-der NPs showed the highest in vitro uptake and anti-inflammatory activity, blunting the secretion of IL-6, TNF-α, and PGE2 cytokines. Moreover, all NPs reduced the production of nitric oxide and NLRP3 inflammasome, and had a stronger anti-inflammatory effect than the major corticosteroid dexamethasone. In particular, the results demonstrate that natural CE protects endothelial cells from inflammatory stress when encapsulated in NPs based on quaternary ammonium chitosan. The CE beneficial effects were directly related with in vitro internalization of CE-loaded NPs. View Full-Text
Keywords: inflammation; sweet cherry (Prunus avium L.); polyphenols; nanoparticles; HUVEC; NLRP3 inflammasome inflammation; sweet cherry (Prunus avium L.); polyphenols; nanoparticles; HUVEC; NLRP3 inflammasome
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MDPI and ACS Style

Beconcini, D.; Felice, F.; Zambito, Y.; Fabiano, A.; Piras, A.M.; Macedo, M.H.; Sarmento, B.; Di Stefano, R. Anti-Inflammatory Effect of Cherry Extract Loaded in Polymeric Nanoparticles: Relevance of Particle Internalization in Endothelial Cells. Pharmaceutics 2019, 11, 500. https://doi.org/10.3390/pharmaceutics11100500

AMA Style

Beconcini D, Felice F, Zambito Y, Fabiano A, Piras AM, Macedo MH, Sarmento B, Di Stefano R. Anti-Inflammatory Effect of Cherry Extract Loaded in Polymeric Nanoparticles: Relevance of Particle Internalization in Endothelial Cells. Pharmaceutics. 2019; 11(10):500. https://doi.org/10.3390/pharmaceutics11100500

Chicago/Turabian Style

Beconcini, Denise; Felice, Francesca; Zambito, Ylenia; Fabiano, Angela; Piras, Anna M.; Macedo, Maria H.; Sarmento, Bruno; Di Stefano, Rossella. 2019. "Anti-Inflammatory Effect of Cherry Extract Loaded in Polymeric Nanoparticles: Relevance of Particle Internalization in Endothelial Cells" Pharmaceutics 11, no. 10: 500. https://doi.org/10.3390/pharmaceutics11100500

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