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Solid dispersions of ursolic acid incorporated in hydrogels to topical administration: development, characterization and in vitro and in vivo biological evaluation

Grant number: 16/22544-0
Support Opportunities:Scholarships in Brazil - Master
Effective date (Start): March 01, 2017
Effective date (End): May 31, 2019
Field of knowledge:Health Sciences - Pharmacy - Pharmaceutical Technology
Acordo de Cooperação: Coordination of Improvement of Higher Education Personnel (CAPES)
Principal Investigator:Marlus Chorilli
Grantee:Andressa Maria Pironi
Host Institution: Faculdade de Ciências Farmacêuticas (FCFAR). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil
Associated scholarship(s):18/17768-2 - In vitro human skin permeation of ursolic acid from solid dispersions carried in poloxamer-based hydrogel, BE.EP.MS


The skin inflammation involves the release of several inflammatory mediators, which in huge amounts can be noxious resulting in a inflammatory and chronic skin diseases, such as atopic dermatitis and psoriasis. The ursolic acid (UA) is a pentacyclic triterpenoid obtained from plant sources and it has a potent anti-inflammatory action by inhibition or reduction of different inflammatory mediators, such as histamine, cytokine secretion (tumor necrosis factor alpha -TNF±, interleukins-IL), ihibition of the activity of 5-lipoxygenase, elastase and synthesis of nitric oxide (ON) and E2 prostaglandins (PGE2), mainly through inhibition of NF-kB, but its low solubility in water limits the therapeutic application. The development of solid dispersions (SD) composed by poloxamer 407 (407P) or D-alpha-tocopheryl polyethylene glycol 1000 succinate associated with colloidal silicon dioxide (TPGS/Aerosil® 200) is an innovative strategy to improve the solubility of AU. Thus, to facilitate the topical administration of DS using hydrogels (HG) of 407P with bioadhesive properties may be interesting, because these systems allow a long time at the local retention of the drug. The objective of the present study is to develope, to characterize and to evaluate the solid dispersion 407P and TPGS/Aerosil®200 for cutaneous administration, relating the cytotoxicity in vitro and anti-inflamatory activity in vivo. The SD will be obtained by the solvent evaporation technique and characterized by analysis of particle size, solubility study, differential scanning calorimetry, X-ray diffraction, electron microscopy and study of physicochemical stability. Moreover, the SD will be incorporated in HG of 407P which will be characterized by texture profile analysis, rheology and in vitro bioadhesion test. The release assays and in vitro skin permeation will be made using SD free and associated with HG. Finally, in vitro biological assays will be performed to assess cytotoxicity of formulation and in vivo activity to evaluate the effect of anti-inflammatory activity of formulations in an animal model, such as, ear edema induced by croton oil. Therefore, it is expected to obtain a novel formulation to delivere the AU to facilitate its use as antiinflammatory in skin diseases. (AU)

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Scientific publications (4)
(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)
PIRONI, ANDRESSA MARIA; DE ARAUJO, PATRICIA ROCHA; FERNANDES, MARIZA AIRES; NUNES SALGADO, HERIDA REGINA; CHORILLI, MARLUS. Characteristics, Biological Properties and Analytical Methods of Ursolic Acid: A Review. CRITICAL REVIEWS IN ANALYTICAL CHEMISTRY, v. 48, n. 1, p. 86-93, . (16/22544-0)
PIRONI, ANDRESSA MARIA; MELERO, ANA; ELOY, JOSIMAR O.; JOSE GUILLOT, ANTONIO; SANTOS, KAIO PINI; CHORILLI, MARLUS. Solid dipersions included in poloxamer hydrogels have favorable rheological properties for topical application and enhance the in vivo antiinflammatory effect of ursolic acid. JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY, v. 74, p. 12-pg., . (16/22544-0, 18/17768-2)
ANDRESSA MARIA PIRONI; JOSIMAR DE OLIVEIRA ELOY; CAMILA FERNANDA RODERO; SELMA GUTIERREZ ANTONIO; JOVAN DURAN ALONSO; MARLUS CHORILLI. PVP solid dispersions containing Poloxamer 407 or TPGS for the improvement of ursolic acid release. Brazilian Journal of Pharmaceutical Sciences, v. 59, . (16/22544-0)
FONSECA-SANTOS, BRUNO; ARAUJO, GIOVANNA ANGELI; FERREIRA, PAULA SCANAVEZ; VICTORELLI, FRANCESCA DAMIANI; PIRONI, ANDRESSA MARIA; ARAUJO, VICTOR HUGO SOUSA; CARVALHO, SUZANA GONCALVES; CHORILLI, MARLUS. Design and Characterization of Lipid-Surfactant-Based Systems for Enhancing Topical Anti-Inflammatory Activity of Ursolic Acid. PHARMACEUTICS, v. 15, n. 2, p. 14-pg., . (17/10016-2, 17/22928-6, 17/23357-2, 19/10761-5, 15/05394-2, 16/22544-0)
Academic Publications
(References retrieved automatically from State of São Paulo Research Institutions)
PIRONI, Andressa Maria. Dispersões sólidas de ácido ursólico veiculadas em hidrogéis para administração cutânea: desenvolvimento, caracterização e avaliação biológica in vitro e in vivo. 2019. Master's Dissertation - Universidade Estadual Paulista (Unesp). Faculdade de Ciências Farmacêuticas. Araraquara Araraquara.

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