Incorporation of Ursolic Acid in Liquid Crystalline Systems Improves the Antifungal Activity Against Candida Sp
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ORIGINAL ARTICLE
Incorporation of Ursolic Acid in Liquid Crystalline Systems Improves the Antifungal Activity Against Candida Sp Gabriel Davi Marena 1 & Bruno Fonseca-Santos 1 & Ramos Matheus Aparecido dos Santos 1 & Karen Cristina dos Santos 1 & Taís Maria Bauab 1 & Marlus Chorilli 1
# Springer Science+Business Media, LLC, part of Springer Nature 2020
Abstract Purpose Infectious diseases caused by Candida sp. have high drug resistance due to the uncontrolled use of antibiotics. Among the natural products, ursolic acid (UA), a triterpene, has been increasing interest due to its antimicrobial effects. However, the physicochemical properties of UA, such as its low aqueous solubility, lead to failure of therapeutic application. Because of this, drug release systems, such as liquid crystals (LCs), can improve solubilization and increase the therapeutic efficacy of many drugs. Methods In this work, we evaluated the antifungal potential of UA and loaded into LC precursor system against Candida sp. The system was composed of oleic acid (30%), polysorbate 80 (60%), and purified water (10%). Polarized light microscopy, rheological assays, and simulated vaginal fluid (SVF) simulations were performed. Cytotoxicity assay was evaluated against L-929 cells (murine fibroblast), and antifungal evaluation was performed by microplate microdilution method against Candida albicans, Candida glabrata, Candida krusei, Candida parapsilosis, and Candida tropicalis. Results The system showed acceptable parameters for UA incorporation, such as adhesiveness, texture, and flow behaviors, compatible to vaginal administration. Free UA showed no antifungal activity; however, after incorporation into LCs, it was observed against C. albicans, C. glabrata, C. tropicalis, and C. parapsilosis (MIC values around 500 μg/mL and 3.9 μg/cell viability assays showed moderate cytotoxicity [halo diameter 1.00 ± 0.156]). Conclusion In conclusion, the results corroborate in the materials field as a possible alternative in the treatment of infectious diseases by Candida species and the systems showed potential promising for enhancing AU antifungal performance with the application on vulvovaginitis. Keywords Fungal infections . Candida species . Ursolic acid . Liquid crystal system . Nanotechnology
Abbreviations AmB Amphotericin B DMEM Culture Medium Dulbecco F Formulation containing 60% (w/w) of surfactant, 30% (w/w) of oleic acid, and 10% (w/w) of purified water F100 Formulation containing 60% (w/w) of surfactant, 30% (w/w) of oleic acid, and 10% (w/w) of Gabriel Davi Marena and Bruno Fonseca-Santos contributed equally to this work.
F30
F50
FLC FUA
* Marlus Chorilli [email protected]
FUA100 1
School of Pharmaceutical Sciences, São Paulo State University (UNESP), Araraquara, São Paulo 14800-903, Brazil
purified water diluted with 100% (v/w) of simulated vaginal fluid Formulation containing 60% (w/w) of surfactant, 30% (w/w) of oleic acid, and 10% (w/w) of purified water diluted with 30% (v/w) of simulated vaginal fluid Formulation containing 60
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