| Autor: |
Beconcini D; Department of Life Sciences, University of Siena, via P.A. Mattioli 4, 53100 Siena, Italy. denisebeconcini@gmail.com.; Department of Pharmacy, University of Pisa, via Bonanno 33, 56100 Pisa, Italy. denisebeconcini@gmail.com.; Cardiovascular Research Laboratory, Department of Surgery, Medical, Molecular, and Critical Area Pathology, University of Pisa, via Paradisa 2, 56100 Pisa, Italy. denisebeconcini@gmail.com., Fabiano A; Department of Pharmacy, University of Pisa, via Bonanno 33, 56100 Pisa, Italy. angela.fabiano@unipi.it., Di Stefano R; Cardiovascular Research Laboratory, Department of Surgery, Medical, Molecular, and Critical Area Pathology, University of Pisa, via Paradisa 2, 56100 Pisa, Italy. rossella.distefano@unipi.it.; Interdepartmental Research Center Nutraceuticals and Food for Health, University of Pisa, via Borghetto 80, 56100 Pisa, Italy. rossella.distefano@unipi.it., Macedo MH; i3S-Instituto de Investigação e Inovação em Saúde, University of Porto, Rua Alfredo Allen 208, 4200-153 Porto, Portugal. helena.macedo@i3s.up.pt.; INEB-Instituto de Engenharia Biomédica, Universidade do Porto, Rua Alfredo Allen, 208, 4200-135 Porto, Portugal. helena.macedo@i3s.up.pt.; ICBAS-Instituto de Ciências Biomédicas Abel Salazar, University of Porto, Rua de Jorge Viterbo Ferreira 228, 4050-313 Porto, Portugal. helena.macedo@i3s.up.pt., Felice F; Cardiovascular Research Laboratory, Department of Surgery, Medical, Molecular, and Critical Area Pathology, University of Pisa, via Paradisa 2, 56100 Pisa, Italy. francesca.felice77@hotmail.it., Zambito Y; Department of Pharmacy, University of Pisa, via Bonanno 33, 56100 Pisa, Italy. ylenia.zambito@unipi.it.; Interdepartmental Research Center Nutraceuticals and Food for Health, University of Pisa, via Borghetto 80, 56100 Pisa, Italy. ylenia.zambito@unipi.it., Sarmento B; i3S-Instituto de Investigação e Inovação em Saúde, University of Porto, Rua Alfredo Allen 208, 4200-153 Porto, Portugal. bruno.sarmento@ineb.up.pt.; INEB-Instituto de Engenharia Biomédica, Universidade do Porto, Rua Alfredo Allen, 208, 4200-135 Porto, Portugal. bruno.sarmento@ineb.up.pt.; CESPU, Instituto de Investigação e Formação Avançada em Ciências e Tecnologias da Saúde, Rua Central de Gandra, 1317, 4585-116 Gandra, Portugal. bruno.sarmento@ineb.up.pt. |
| Abstrakt: |
Polyphenolic compounds contained in cherry extract (CE) are well known for their antioxidant and anti-inflammatory properties. Unfortunately, most of these natural compounds have low oral bioavailability, reducing their widespread use. Here, different concentrations of polyphenol-rich CE from Tuscany (Italy), encapsulated in poly(lactic- co -glycolic acid) (PLGA) nanoparticles (NPs), were compared with those encapsulated in two NP types, different from each other in terms of mucoadhesivity, obtained with chitosan derivatives (Ch-der), regarding CE gastrointestinal (GI) permeability and protective effect on oxidative stress. Different NP systems were physico-chemically characterized, and the antioxidant GI permeability was evaluated in a triple-cell co-culture model (Caco-2/HT29-MTX/Raji B), resembling the intestine. PLGA NPs efficiently entrapped CE (up to 840 µg gallic acid equivalent (GAE)/mL) without altering size (210 nm), polydispersity index (0.05), or zeta potential (-10.7 mV). Such NPs promoted permeation of encapsulated CE at a CE polyphenolic concentration of at least 2 µg GAE/mL. More mucoadhesive NPs from Ch-der, coded quaternary ammonium S-protected thiolated chitosan (QA-Ch-S-pro) NP, promoted CE GI permeation of 0.5 µg GAE/mL. At higher concentrations of Ch-der polymers, the resulting NPs containing CE were toxic toward Caco-2 and HT29-MTX cells. CE protected human umbilical vein endothelial cells (HUVECs) from oxidative stress and maintained its activity when entrapped in PLGA NPs. CE encapsulated in QA-Ch-S-pro NP protected HUVECs from oxidative stress, even more effectively than non-encapsulated CE. Furthermore, mucoadhesive NPs from Ch-der were more effective antioxidant protectors than PLGA NPs, but less cytotoxic PLGA NPs could be more useful when comparatively high therapeutic antioxidant doses are needed. |
