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Mucoadhesive precursor systems of liquids crystals for buccal administration of curcumin associated with photodynamic therapy in the treatment of oral candidiasis

Grant number: 14/22045-9
Support Opportunities:Scholarships in Brazil - Doctorate
Effective date (Start): July 01, 2015
Effective date (End): January 31, 2018
Field of knowledge:Health Sciences - Pharmacy - Pharmaceutical Technology
Acordo de Cooperação: Coordination of Improvement of Higher Education Personnel (CAPES)
Principal Investigator:Marlus Chorilli
Grantee:Jéssica Bernegossi
Host Institution: Faculdade de Ciências Farmacêuticas (FCFAR). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil
Associated scholarship(s):16/14167-2 - Evaluation of in vitro biocompatibility and cellular uptake of a curcumin-loaded liquid crystal precursor mucoadhesive system with or without light activation., BE.EP.DR


The oral candidiasis (OC) is caused by infection the yeast Candida ssp. in soft tissues of the oral cavity, being due mainly of imbalance in the oral microbiota, changes in pH and salivary flow. The treatment of choice involves the administration of topical antifungals or systemic, for which we have observed numerous cases of resistance. In this way, many researchers are working the use of alternative methods, as Photodynamic therapy (PDT), and in the discovery of substances, among them those from natural sources, that may present therapeutic interest in the treatment of OC. Curcumin (CUR), naturally occurring compound isolated from Rhizomes of Curcuma longa, has shown antifungal activity, being this effect potentiated by the use of PDT, once operates also as photosensitizer. However, its clinical use faces many challenges, due mainly to its physicochemical characteristics, as low solubility in aqueous acid pH conditions and physiological, rapid hydrolysis in alkaline pH and instability in the presence of light, resulting including pharmacokinetic restrictions, such as low oral absorption, extensive hepatic metabolism and quick elimination. Soon, its incorporation in nanostructured precursor systems of liquids crystals incorporated mucoadhesive polymeric admixtures for oral administration proves to be an interesting option to enable its use, associated or not to PDT, since these systems can protect the drug degradation and increase the length of stay of the formulation in oral environment, enabling a controlled release in the specific site of action. Besides, oral administration may be advantageous, once the oral mucosa features high permeability, high blood flow and the absence of first-pass metabolism, optimizing the drug action. This project aims to evaluate the potential of precursor systems of liquids crystals mucoadhesive for oral administration of CUR, as well as check the potentiation of the treatment of OC with the use of PDT, employing in vitro and in vivo studies of their activity and effectiveness. The precursor systems of liquids crystals incorporated CUR will be characterized employing polarized light microscopy, rheology, Small-angle X-ray scattering (SAXS), texture profile analysis with simulated saliva solution and in vitro mucoadhesion. Will be developed and validated analytical methodology for quantification of CUR release studies and systems, in vitro permeation and retention. They will be carried out biological assay in vitro of antimicrobial activity against the biofilm, cytotoxicity and uptake cellular of CUR incorporated or not in precursor systems of liquids crystals. Finally, they will be carried out in vivo assays. (AU)

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Scientific publications
(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)
BERNEGOSSI, JESSICA; FONTANA, CARLA RAQUEL; CAIAFFA, KARINA SAMPAIO; DUQUE, CRISTIANE; CHORILLI, MARLUS. Inhibitory Effect of a KSL-W Peptide-Loaded Poloxamer 407-Based Microemulsions for Buccal Delivery on Fusobacterium nucleatum Biofilm. JOURNAL OF BIOMEDICAL NANOTECHNOLOGY, v. 16, n. 3, p. 390-397, . (14/22045-9)
MIYASHIRO, C. A.; BERNEGOSSI, J.; BONIFACIO, V, B.; DE TOLEDO, L. G.; RAMOS, M. A. S.; BAUAB, T. M.; CHORILLI, M.. Development and characterization of a novel liquid crystalline system containing sodium alginate for incorporation of trans-resveratrol intended for treatment of buccal candidiasis. Pharmazie, v. 75, n. 5, p. 179-185, . (14/22045-9)
Academic Publications
(References retrieved automatically from State of São Paulo Research Institutions)
BERNEGOSSI, Jéssica. Mucoadhesive precursor systems of liquids crystals for buccal admnistration of curcumin associated with photodynamic therapy in the treatment of oral candidiasis.. 2018. Doctoral Thesis - Universidade Estadual Paulista (Unesp). Faculdade de Ciências Farmacêuticas. Araraquara Araraquara.

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