Novel resveratrol nanodelivery systems based on lipid nanoparticles to enhance its oral bioavailability

Ana Rute Neves,1 Marlene L&uacute;cio,1 Susana Martins,2,3 Jos&eacute; Lu&iacute;s Costa Lima,1 Salette Reis11REQUIMTE, Chemistry Department, Faculty of Pharmacy, University of Porto, 2Laboratory for Pharmaceutical Technology/Research Centre in Pharmaceutical Sciences, Facult...

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Autores principales:	Neves AR, L&uacute;cio M, Martins S, Lima JL, Reis S
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Lenguaje:	EN
Publicado:	Dove Medical Press 2013
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/57fee4ca1e2d429fa1fce518f011c7a8
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spelling	oai:doaj.org-article:57fee4ca1e2d429fa1fce518f011c7a82021-12-02T05:10:00ZNovel resveratrol nanodelivery systems based on lipid nanoparticles to enhance its oral bioavailability1176-91141178-2013https://doaj.org/article/57fee4ca1e2d429fa1fce518f011c7a82013-01-01T00:00:00Zhttp://www.dovepress.com/novel-resveratrol-nanodelivery-systems-based-on-lipid-nanoparticles-to-a11880https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Ana Rute Neves,1 Marlene L&uacute;cio,1 Susana Martins,2,3 Jos&eacute; Lu&iacute;s Costa Lima,1 Salette Reis11REQUIMTE, Chemistry Department, Faculty of Pharmacy, University of Porto, 2Laboratory for Pharmaceutical Technology/Research Centre in Pharmaceutical Sciences, Faculty of Pharmacy, University of Porto, 3Institute of Biomedical Engineering, University of Porto, PortugalIntroduction: Resveratrol is a polyphenol found in grapes and red wines. Interest in this polyphenol has increased due to its pharmacological cardio- and neuroprotective, chemopreventive, and antiaging effects, among others. Nevertheless, its pharmacokinetic properties are less favorable, since the compound has poor bioavailability, low water solubility, and is chemically unstable. To overcome these problems, we developed two novel resveratrol nanodelivery systems based on lipid nanoparticles to enhance resveratrol&#39;s oral bioavailability for further use in medicines, supplements, and nutraceuticals.Methods and materials: Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) loaded with resveratrol were successfully produced by a modified hot homogenization technique. These were completely characterized to evaluate the quality of the developed resveratrol-loaded nanoparticles.Results: Cryo-scanning electron microscopy morphology studies showed spherical and uniform nanoparticles with a smooth surface. An average resveratrol entrapment efficiency of ~70% was obtained for both SLNs and NLCs. Dynamic light scattering measurements gave a Z-average of 150&ndash;250 nm, polydispersity index of ~0.2, and a highly negative zeta potential of around &minus;30 mV with no statistically significant differences in the presence of resveratrol. These characteristics remained unchanged for at least 2 months, suggesting good stability. Differential scanning calorimetry studies confirmed the solid state of the SLNs and NLCs at both room and body temperatures. The NLCs had a less ordered crystalline structure conferred by the inclusion of the liquid lipid, since they had lower values for phase transition temperature, melting enthalpy, and the recrystallization index. The presence of resveratrol induced a disorder in the crystal structure of the nanoparticles, suggesting a favoring of its entrapment. The in vitro release studies on conditions of storage showed a negligible resveratrol release over several hours for both nanosystems and the in vitro simulation of gastrointestinal transit showed that the resveratrol remained mostly associated with the lipid nanoparticles after their incubation in digestive fluids.Conclusion: Both nanodelivery systems can be considered suitable carriers for oral administration, conferring protection to the incorporated resveratrol and allowing a controlled release after uptake.Keywords: nanodelivery systems, solid lipid nanoparticles, nanostructured lipid carriers, polyphenolNeves ARL&uacute;cio MMartins SLima JLReis SDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2013, Iss default, Pp 177-187 (2013)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Neves AR L&uacute;cio M Martins S Lima JL Reis S Novel resveratrol nanodelivery systems based on lipid nanoparticles to enhance its oral bioavailability
description	Ana Rute Neves,1 Marlene L&uacute;cio,1 Susana Martins,2,3 Jos&eacute; Lu&iacute;s Costa Lima,1 Salette Reis11REQUIMTE, Chemistry Department, Faculty of Pharmacy, University of Porto, 2Laboratory for Pharmaceutical Technology/Research Centre in Pharmaceutical Sciences, Faculty of Pharmacy, University of Porto, 3Institute of Biomedical Engineering, University of Porto, PortugalIntroduction: Resveratrol is a polyphenol found in grapes and red wines. Interest in this polyphenol has increased due to its pharmacological cardio- and neuroprotective, chemopreventive, and antiaging effects, among others. Nevertheless, its pharmacokinetic properties are less favorable, since the compound has poor bioavailability, low water solubility, and is chemically unstable. To overcome these problems, we developed two novel resveratrol nanodelivery systems based on lipid nanoparticles to enhance resveratrol&#39;s oral bioavailability for further use in medicines, supplements, and nutraceuticals.Methods and materials: Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) loaded with resveratrol were successfully produced by a modified hot homogenization technique. These were completely characterized to evaluate the quality of the developed resveratrol-loaded nanoparticles.Results: Cryo-scanning electron microscopy morphology studies showed spherical and uniform nanoparticles with a smooth surface. An average resveratrol entrapment efficiency of ~70% was obtained for both SLNs and NLCs. Dynamic light scattering measurements gave a Z-average of 150&ndash;250 nm, polydispersity index of ~0.2, and a highly negative zeta potential of around &minus;30 mV with no statistically significant differences in the presence of resveratrol. These characteristics remained unchanged for at least 2 months, suggesting good stability. Differential scanning calorimetry studies confirmed the solid state of the SLNs and NLCs at both room and body temperatures. The NLCs had a less ordered crystalline structure conferred by the inclusion of the liquid lipid, since they had lower values for phase transition temperature, melting enthalpy, and the recrystallization index. The presence of resveratrol induced a disorder in the crystal structure of the nanoparticles, suggesting a favoring of its entrapment. The in vitro release studies on conditions of storage showed a negligible resveratrol release over several hours for both nanosystems and the in vitro simulation of gastrointestinal transit showed that the resveratrol remained mostly associated with the lipid nanoparticles after their incubation in digestive fluids.Conclusion: Both nanodelivery systems can be considered suitable carriers for oral administration, conferring protection to the incorporated resveratrol and allowing a controlled release after uptake.Keywords: nanodelivery systems, solid lipid nanoparticles, nanostructured lipid carriers, polyphenol
format	article
author	Neves AR L&uacute;cio M Martins S Lima JL Reis S
author_facet	Neves AR L&uacute;cio M Martins S Lima JL Reis S
author_sort	Neves AR
title	Novel resveratrol nanodelivery systems based on lipid nanoparticles to enhance its oral bioavailability
title_short	Novel resveratrol nanodelivery systems based on lipid nanoparticles to enhance its oral bioavailability
title_full	Novel resveratrol nanodelivery systems based on lipid nanoparticles to enhance its oral bioavailability
title_fullStr	Novel resveratrol nanodelivery systems based on lipid nanoparticles to enhance its oral bioavailability
title_full_unstemmed	Novel resveratrol nanodelivery systems based on lipid nanoparticles to enhance its oral bioavailability
title_sort	novel resveratrol nanodelivery systems based on lipid nanoparticles to enhance its oral bioavailability
publisher	Dove Medical Press
publishDate	2013
url	https://doaj.org/article/57fee4ca1e2d429fa1fce518f011c7a8
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Novel resveratrol nanodelivery systems based on lipid nanoparticles to enhance its oral bioavailability

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