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Improving Drug Delivery on Candida Albicans Using Geraniol Nanoemulsion

Geraniol (GE) is a monoterpene alcohol with excellent antifungal activity. However, its low solubility and high volatility impair its use. Nanoemulsions (NE) are excellent delivery systems for poorly soluble and volatile drugs, achieving controlled release of the active ingredient. The aim of this s...

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Autores principales: Silva Pontes, Cristiano, Garcia de Carvalho, Gabriel, Rosa Perin Leite, Andressa, Chorilli, Marlus, Palomari Spolidorio, Denise Madalena
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10609964/
https://www.ncbi.nlm.nih.gov/pubmed/37896235
http://dx.doi.org/10.3390/pharmaceutics15102475
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author Silva Pontes, Cristiano
Garcia de Carvalho, Gabriel
Rosa Perin Leite, Andressa
Chorilli, Marlus
Palomari Spolidorio, Denise Madalena
author_facet Silva Pontes, Cristiano
Garcia de Carvalho, Gabriel
Rosa Perin Leite, Andressa
Chorilli, Marlus
Palomari Spolidorio, Denise Madalena
author_sort Silva Pontes, Cristiano
collection PubMed
description Geraniol (GE) is a monoterpene alcohol with excellent antifungal activity. However, its low solubility and high volatility impair its use. Nanoemulsions (NE) are excellent delivery systems for poorly soluble and volatile drugs, achieving controlled release of the active ingredient. The aim of this study was to improve the delivery of geraniol (GE) incorporated in NE against Candida albicans in order to evaluate the antibiofilm effect and cytotoxicity. Nanoemulsion containing 10% oil phase (cholesterol) (w/w), 10% surfactant (mixture of soy phosphatidylcholine and Brij 58; 1:2) (w/w), and 80% aqueous phase (phosphate buffer) (w/w) was synthesized. Incorporation of GE was carried out by sonication and the final compounds were characterized by hydrodynamic diameter, polydispersity index (PDI), and zeta potential (ZP), in addition to evaluation of physicochemical stability after 6 months and 1 year. The GE-NE effect was evaluated on Candida albicans biofilms and cytotoxic effect was evaluated on immortalized normal oral cell line NOK-Si. The diameter of GE-NE was 232.3 ± 2.7 nm and PDI 0.155 with exhibited homogeneity and stability in solution. GE-NE showed antibiofilm activity at a concentration of 75 μg/mL with reduction of >6.0 log(10), and no cytotoxicity against NOK-Si cells at concentrations below 150 μg/mL was observed. GE-NE proved to be a promising candidate for prevention and treatment of fungal diseases.
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spelling pubmed-106099642023-10-28 Improving Drug Delivery on Candida Albicans Using Geraniol Nanoemulsion Silva Pontes, Cristiano Garcia de Carvalho, Gabriel Rosa Perin Leite, Andressa Chorilli, Marlus Palomari Spolidorio, Denise Madalena Pharmaceutics Article Geraniol (GE) is a monoterpene alcohol with excellent antifungal activity. However, its low solubility and high volatility impair its use. Nanoemulsions (NE) are excellent delivery systems for poorly soluble and volatile drugs, achieving controlled release of the active ingredient. The aim of this study was to improve the delivery of geraniol (GE) incorporated in NE against Candida albicans in order to evaluate the antibiofilm effect and cytotoxicity. Nanoemulsion containing 10% oil phase (cholesterol) (w/w), 10% surfactant (mixture of soy phosphatidylcholine and Brij 58; 1:2) (w/w), and 80% aqueous phase (phosphate buffer) (w/w) was synthesized. Incorporation of GE was carried out by sonication and the final compounds were characterized by hydrodynamic diameter, polydispersity index (PDI), and zeta potential (ZP), in addition to evaluation of physicochemical stability after 6 months and 1 year. The GE-NE effect was evaluated on Candida albicans biofilms and cytotoxic effect was evaluated on immortalized normal oral cell line NOK-Si. The diameter of GE-NE was 232.3 ± 2.7 nm and PDI 0.155 with exhibited homogeneity and stability in solution. GE-NE showed antibiofilm activity at a concentration of 75 μg/mL with reduction of >6.0 log(10), and no cytotoxicity against NOK-Si cells at concentrations below 150 μg/mL was observed. GE-NE proved to be a promising candidate for prevention and treatment of fungal diseases. MDPI 2023-10-17 /pmc/articles/PMC10609964/ /pubmed/37896235 http://dx.doi.org/10.3390/pharmaceutics15102475 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Silva Pontes, Cristiano
Garcia de Carvalho, Gabriel
Rosa Perin Leite, Andressa
Chorilli, Marlus
Palomari Spolidorio, Denise Madalena
Improving Drug Delivery on Candida Albicans Using Geraniol Nanoemulsion
title Improving Drug Delivery on Candida Albicans Using Geraniol Nanoemulsion
title_full Improving Drug Delivery on Candida Albicans Using Geraniol Nanoemulsion
title_fullStr Improving Drug Delivery on Candida Albicans Using Geraniol Nanoemulsion
title_full_unstemmed Improving Drug Delivery on Candida Albicans Using Geraniol Nanoemulsion
title_short Improving Drug Delivery on Candida Albicans Using Geraniol Nanoemulsion
title_sort improving drug delivery on candida albicans using geraniol nanoemulsion
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10609964/
https://www.ncbi.nlm.nih.gov/pubmed/37896235
http://dx.doi.org/10.3390/pharmaceutics15102475
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