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Liquid crystalline systems as potential strategy ofr incorporation of trans-resveratrol: development, physicochemical characterization and in vitro and in vivo biological assays

Grant number: 14/24180-0
Support Opportunities:Regular Research Grants
Duration: August 01, 2015 - July 31, 2017
Field of knowledge:Health Sciences - Pharmacy - Pharmaceutical Technology
Principal Investigator:Marlus Chorilli
Grantee:Marlus Chorilli
Host Institution: Faculdade de Ciências Farmacêuticas (FCFAR). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil
Associated researchers:Maria Palmira Daflon Gremião ; Rúbia Casagrande


The daily exposure of the skin to ultraviolet (UV) radiation can cause direct damage to DNA and cause the proliferation of reactive oxygen species (ROS), which leads to an imbalance between free radicals and antioxidant enzymes in the epidermis, such as superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPx). This imbalance leads to a state of oxidative stress, which can unleash a number of skin disorders, among them skin cancer. Research has shown that trans-resveratrol (RES), due to their anti-inflammatory, antioxidant and chemopreventive properties, is a potential active substance in therapy against changes resulting from oxidative stress. However, some of their physicochemical properties, such as limited aqueous solubility, make their effectiveness on therapeutic cutaneous more difficult since it has low penetration into the skin. Thus, the use of nanostructured delivery systems for cutaneous administration of the RES, such as liquid-crystalline systems (LCS) would be extremely viable due to its characteristics of interaction with the stratum corneum and other skin layers and capacity of drug arrangement with protective effect and sustainer of release. The objectives of this work are to develop LCS to incorporate the RES and to characterize them by means of polarized light microscopy, small-angle X-ray scattering (SAXS), rheology, thermal analysis, texture profile and in vitro bioadhesion. Release, retention and permeation tests will be performed in vitro using skin of an animal model. Subsequently, in vitro cytotoxicty will be performed and the in vivo anti-inflammatory and antioxidant effectiveness will be verified by model of stress oxidative cutaneous induced by UVB radiation. From the results obtained in this project, it is expected to obtain innovative systems that can be an alternative to treat skin disorders resulting from oxidative stress, contributing to technological and scientific improvement of the country through the development of new nanostructured drug delivery systems that may be accessible to the population. (AU)

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Scientific publications (9)
(References retrieved automatically from Web of Science and SciELO through information on FAPESP grants and their corresponding numbers as mentioned in the publications by the authors)
FONSECA-SANTOS, BRUNO; SILVA, PATRICIA BENTO; RIGON, ROBERTA BALASIN; SATO, MARIANA RILLO; CHORILLI, MARIUS. Formulating SLN and NLC as Innovative Drug Delivery Systems for Non-Invasive Routes of Drug Administration. Current Medicinal Chemistry, v. 27, n. 22, p. 3623-3656, . (15/05394-2, 13/09265-7, 14/24180-0, 13/21500-1, 16/11198-4)
FONSECA-SANTOS, BRUNO; SATAKE, CINTHIA YUKA; FIORAMONTI CALIXTO, GIOVANA MARIA; DOS SANTOS, ALINE MARTINS; CHORILLI, MARLUS. Trans-resveratrol-loaded nonionic lamellar liquid-crystalline systems: structural, rheological, mechanical, textural, and bioadhesive characterization and evaluation of in vivo anti-inflammatory activity. INTERNATIONAL JOURNAL OF NANOMEDICINE, v. 12, p. 6883-6893, . (14/24180-0)
FONSECA-SANTOS, BRUNO; CHORILLI, MARLUS. The uses of resveratrol for neurological diseases treatment and insights for nanotechnology based-drug delivery systems. International Journal of Pharmaceutics, v. 589, . (15/05394-2, 12/19568-4, 14/24180-0)
DA SILVA, PATRICIA BENTO; FIORAMONTI CALIXTO, GIOVANA MARIA; OSHIRO JUNIOR, JOAO AUGUSTO; AVILA BOMBARDELLI, RAISA LANA; FONSECA-SANTOS, BRUNO; RODERO, CAMILA FERNANDA; CHORILLI, MARLUS. Structural Features and the Anti-Inflammatory Effect of Green Tea Extract-Loaded Liquid Crystalline Systems Intended for Skin Delivery. POLYMERS, v. 9, n. 1, . (14/24180-0)
OYAFUSO, MARCIA H.; CARVALHO, FLAVIA C.; TAKESHITA, TATIANE M.; DE SOUZA, ANA L. RIBEIRO; ARAUJO, DANIELE R.; MERINO, VIRGINIA; GREMIAO, MARIA PALMIRA D.; CHORILLI, MARLUS. Development and In Vitro Evaluation of Lyotropic Liquid Crystals for the Controlled Release of Dexamethasone. POLYMERS, v. 9, n. 8, . (10/17037-6, 14/24180-0)
MONTEIRO E SILVA, SILAS ARANDAS; FIORAMONTI CALIXTO, GIOVANA MARIA; CAJADO, JULIANA; ANTUNES DE CARVALHO, PATRICIA CABALLIERI; RODERO, CAMILA FERNANDA; CHORILLI, MARLUS; LEONARDI, GISLAINE RICCI. Gallic Acid-Loaded Gel Formulation Combats Skin Oxidative Stress: Development, Characterization and Ex Vivo Biological Assays. POLYMERS, v. 9, n. 9, . (13/01565-1, 13/01118-5, 11/04908-1, 14/24180-0)
FONSECA-SANTOS, BRUNO; CHORILLI, MARLUS. An overview of carboxymethyl derivatives of chitosan: Their use as biomaterials and drug delivery systems. Materials Science & Engineering C-Materials for Biological Applications, v. 77, p. 1349-1362, . (15/05394-2, 14/24180-0)
HONORATO GATTI, TIAGO HENRIQUE; ELOY, JOSIMAR OLIVEIRA; BARBOZA FERREIRA, LEONARDO MIZIARA; DA SILVA, ISABEL CRISTINE; PAVAN, FERNANDO ROGERIO; DAFLON GREMIAO, MARIA PALMIRA; CHORILLI, MARLUS. Insulin-loaded polymeric mucoadhesive nanoparticles: development, characterization and cytotoxicity evaluation. Brazilian Journal of Pharmaceutical Sciences, v. 54, n. 1, . (14/24180-0)
FUJIMURA, ANDRESSA T.; MARTINEZ, RENATA M.; PINHO-RIBEIRO, FELIPE A.; LOPES DIAS DA SILVA, AMELIA M.; BARACAT, MARCELA M.; GEORGETTI, SANDRA R.; VERRI, JR., WALDICEU A.; CHORILLI, MARLUS; CASAGRANDE, RUBIA. Resveratrol-Loaded Liquid-Crystalline System Inhibits UVB-Induced Skin Inflammation and Oxidative Stress in Mice. Journal of Natural Products, v. 79, n. 5, p. 1329-1338, . (14/24180-0, 12/16956-3)

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Filed patent(s) as a result of this research project

COMPOSIÇÃO FARMACÊUTICA E USO DA MESMA BR1020150227060 - Universidade Estadual Paulista (UNESP) . Marlus Chorilli ; Andressa Terumi Fujimura ; Rubia Casagrande ; Renata Micheli Martinez - September 2015, 11