Skin Delivery and in Vitro Biological Evaluation of Trans-Resveratrol-Loaded Solid Lipid Nanoparticles for Skin Disorder Therapies

The aim of this study was to evaluate the skin delivery and in vitro biological activity of trans-resveratrol (RES)-loaded solid lipid nanoparticles (SLNs). The SLNs were composed of stearic acid, poloxamer 407, soy phosphatidylcholine (SPC), an aqueous phase and 0.1% RES. The particle size, polydis...

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Main Authors: Roberta B. Rigon, Naiara Fachinetti, Patrícia Severino, Maria H. A. Santana, Marlus Chorilli
Format: Article
Language:English
Published: MDPI AG 2016-01-01
Series:Molecules
Subjects:
Online Access:http://www.mdpi.com/1420-3049/21/1/116
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spelling doaj-37cd0bdd9b5545e59eb772657dc7654d2020-11-25T00:50:53ZengMDPI AGMolecules1420-30492016-01-0121111610.3390/molecules21010116molecules21010116Skin Delivery and in Vitro Biological Evaluation of Trans-Resveratrol-Loaded Solid Lipid Nanoparticles for Skin Disorder TherapiesRoberta B. Rigon0Naiara Fachinetti1Patrícia Severino2Maria H. A. Santana3Marlus Chorilli4Faculdade de Ciências Farmacêuticas, UNESP—Universidade Estadual Paulista, Campus Araraquara, Departamento de Fármacos e Medicamentos, Araraquara, SP 14800-850, BrazilFaculdade de Ciências Farmacêuticas, UNESP—Universidade Estadual Paulista, Campus Araraquara, Departamento de Fármacos e Medicamentos, Araraquara, SP 14800-850, BrazilCentro de Ciências Biológicas e da Saúde, Universidade Tiradentes, Aracaju, SE 49010-390, BrazilFaculdade de Engenharia Química, Universidade Estadual de Campinas, Campinas, SP 13083-970, BrazilFaculdade de Ciências Farmacêuticas, UNESP—Universidade Estadual Paulista, Campus Araraquara, Departamento de Fármacos e Medicamentos, Araraquara, SP 14800-850, BrazilThe aim of this study was to evaluate the skin delivery and in vitro biological activity of trans-resveratrol (RES)-loaded solid lipid nanoparticles (SLNs). The SLNs were composed of stearic acid, poloxamer 407, soy phosphatidylcholine (SPC), an aqueous phase and 0.1% RES. The particle size, polydispersity index (PdI) and zeta potential were analyzed by dynamic light scattering (DLS). The SLNs were analyzed by scanning electron microscopy (SEM-FEG) and differential scanning calorimetry (DSC). In vitro RES-SLN skin permeation/retention assays were conducted, and their tyrosinase inhibitory activity was evaluated. An MTT reduction assay was performed on HaCat keratinocytes to determine in vitro cytotoxicity. The formulations had average diameter lower than 200 nm, the addition of SPC promoted increases in PdI in the RES-SLNs, but decreases PdI in the RES-free SLNs and the formulations exhibited zeta potentials smaller than −3 mV. The DSC analysis of the SLNs showed no endothermic peak attributable to RES. Microscopic analysis suggests that the materials formed had nanometric size distribution. Up to 45% of the RES permeated through the skin after 24 h. The RES-loaded SLNs were more effective than kojic acid at inhibiting tyrosinase and proved to be non-toxic in HaCat keratinocytes. The results suggest that the investigated RES-loaded SLNs have potential use in skin disorder therapies.http://www.mdpi.com/1420-3049/21/1/116drug delivery systemskin disorderspermeationsolid lipid nanoparticletrans-resveratroltyrosinase
collection DOAJ
language English
format Article
sources DOAJ
author Roberta B. Rigon
Naiara Fachinetti
Patrícia Severino
Maria H. A. Santana
Marlus Chorilli
spellingShingle Roberta B. Rigon
Naiara Fachinetti
Patrícia Severino
Maria H. A. Santana
Marlus Chorilli
Skin Delivery and in Vitro Biological Evaluation of Trans-Resveratrol-Loaded Solid Lipid Nanoparticles for Skin Disorder Therapies
Molecules
drug delivery system
skin disorders
permeation
solid lipid nanoparticle
trans-resveratrol
tyrosinase
author_facet Roberta B. Rigon
Naiara Fachinetti
Patrícia Severino
Maria H. A. Santana
Marlus Chorilli
author_sort Roberta B. Rigon
title Skin Delivery and in Vitro Biological Evaluation of Trans-Resveratrol-Loaded Solid Lipid Nanoparticles for Skin Disorder Therapies
title_short Skin Delivery and in Vitro Biological Evaluation of Trans-Resveratrol-Loaded Solid Lipid Nanoparticles for Skin Disorder Therapies
title_full Skin Delivery and in Vitro Biological Evaluation of Trans-Resveratrol-Loaded Solid Lipid Nanoparticles for Skin Disorder Therapies
title_fullStr Skin Delivery and in Vitro Biological Evaluation of Trans-Resveratrol-Loaded Solid Lipid Nanoparticles for Skin Disorder Therapies
title_full_unstemmed Skin Delivery and in Vitro Biological Evaluation of Trans-Resveratrol-Loaded Solid Lipid Nanoparticles for Skin Disorder Therapies
title_sort skin delivery and in vitro biological evaluation of trans-resveratrol-loaded solid lipid nanoparticles for skin disorder therapies
publisher MDPI AG
series Molecules
issn 1420-3049
publishDate 2016-01-01
description The aim of this study was to evaluate the skin delivery and in vitro biological activity of trans-resveratrol (RES)-loaded solid lipid nanoparticles (SLNs). The SLNs were composed of stearic acid, poloxamer 407, soy phosphatidylcholine (SPC), an aqueous phase and 0.1% RES. The particle size, polydispersity index (PdI) and zeta potential were analyzed by dynamic light scattering (DLS). The SLNs were analyzed by scanning electron microscopy (SEM-FEG) and differential scanning calorimetry (DSC). In vitro RES-SLN skin permeation/retention assays were conducted, and their tyrosinase inhibitory activity was evaluated. An MTT reduction assay was performed on HaCat keratinocytes to determine in vitro cytotoxicity. The formulations had average diameter lower than 200 nm, the addition of SPC promoted increases in PdI in the RES-SLNs, but decreases PdI in the RES-free SLNs and the formulations exhibited zeta potentials smaller than −3 mV. The DSC analysis of the SLNs showed no endothermic peak attributable to RES. Microscopic analysis suggests that the materials formed had nanometric size distribution. Up to 45% of the RES permeated through the skin after 24 h. The RES-loaded SLNs were more effective than kojic acid at inhibiting tyrosinase and proved to be non-toxic in HaCat keratinocytes. The results suggest that the investigated RES-loaded SLNs have potential use in skin disorder therapies.
topic drug delivery system
skin disorders
permeation
solid lipid nanoparticle
trans-resveratrol
tyrosinase
url http://www.mdpi.com/1420-3049/21/1/116
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