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Permeability Characteristics of a New Antifungal Topical Amphotericin B Formulation with γ-Cyclodextrins

Amphotericin B is a low soluble broad-spectrum antifungal agent. Cyclodextrins can be added to amphotericin formulations to enhance both their solubility and antifungal properties. Semisolid amphotericin formulations containing gamma cyclodextrin (AGCD) were prepared and compared with two reference...

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Autores principales: López-Castillo, Carmen, Rodríguez-Fernández, Carmina, Córdoba, Manuel, Torrado, Juan J.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6321561/
https://www.ncbi.nlm.nih.gov/pubmed/30567325
http://dx.doi.org/10.3390/molecules23123349
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author López-Castillo, Carmen
Rodríguez-Fernández, Carmina
Córdoba, Manuel
Torrado, Juan J.
author_facet López-Castillo, Carmen
Rodríguez-Fernández, Carmina
Córdoba, Manuel
Torrado, Juan J.
author_sort López-Castillo, Carmen
collection PubMed
description Amphotericin B is a low soluble broad-spectrum antifungal agent. Cyclodextrins can be added to amphotericin formulations to enhance both their solubility and antifungal properties. Semisolid amphotericin formulations containing gamma cyclodextrin (AGCD) were prepared and compared with two reference formulations—one of them without any solubility enhancer (A) and the other with DMSO (ADMSO). Rheological, the permeability through hairless mouse skin and antifungal characteristics of the different formulations were evaluated. All three semisolid formulations show low thixotropy characteristics. ADMSO was the formulation with the least consistency, lowest viscosity, and greatest extensibility. The AGCD formulation had the opposite behavior and had both the greatest consistency and viscosity and the lowest extensibility. The lowest permeability was obtained with the reference A formulation while both AGCD and ADMSO had a similar permeability enhancement. According to the antimicrobial in vitro efficacy trials, the AGCD formulation showed 45–60% more activity than the reference A formulation. It can be concluded that γ-cyclodextrin is a useful excipient to improve the solubility, permeability, and antifungal activity of amphotericin B in semisolid topical formulations.
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spelling pubmed-63215612019-01-14 Permeability Characteristics of a New Antifungal Topical Amphotericin B Formulation with γ-Cyclodextrins López-Castillo, Carmen Rodríguez-Fernández, Carmina Córdoba, Manuel Torrado, Juan J. Molecules Article Amphotericin B is a low soluble broad-spectrum antifungal agent. Cyclodextrins can be added to amphotericin formulations to enhance both their solubility and antifungal properties. Semisolid amphotericin formulations containing gamma cyclodextrin (AGCD) were prepared and compared with two reference formulations—one of them without any solubility enhancer (A) and the other with DMSO (ADMSO). Rheological, the permeability through hairless mouse skin and antifungal characteristics of the different formulations were evaluated. All three semisolid formulations show low thixotropy characteristics. ADMSO was the formulation with the least consistency, lowest viscosity, and greatest extensibility. The AGCD formulation had the opposite behavior and had both the greatest consistency and viscosity and the lowest extensibility. The lowest permeability was obtained with the reference A formulation while both AGCD and ADMSO had a similar permeability enhancement. According to the antimicrobial in vitro efficacy trials, the AGCD formulation showed 45–60% more activity than the reference A formulation. It can be concluded that γ-cyclodextrin is a useful excipient to improve the solubility, permeability, and antifungal activity of amphotericin B in semisolid topical formulations. MDPI 2018-12-18 /pmc/articles/PMC6321561/ /pubmed/30567325 http://dx.doi.org/10.3390/molecules23123349 Text en © 2018 by the authors. 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 (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
López-Castillo, Carmen
Rodríguez-Fernández, Carmina
Córdoba, Manuel
Torrado, Juan J.
Permeability Characteristics of a New Antifungal Topical Amphotericin B Formulation with γ-Cyclodextrins
title Permeability Characteristics of a New Antifungal Topical Amphotericin B Formulation with γ-Cyclodextrins
title_full Permeability Characteristics of a New Antifungal Topical Amphotericin B Formulation with γ-Cyclodextrins
title_fullStr Permeability Characteristics of a New Antifungal Topical Amphotericin B Formulation with γ-Cyclodextrins
title_full_unstemmed Permeability Characteristics of a New Antifungal Topical Amphotericin B Formulation with γ-Cyclodextrins
title_short Permeability Characteristics of a New Antifungal Topical Amphotericin B Formulation with γ-Cyclodextrins
title_sort permeability characteristics of a new antifungal topical amphotericin b formulation with γ-cyclodextrins
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6321561/
https://www.ncbi.nlm.nih.gov/pubmed/30567325
http://dx.doi.org/10.3390/molecules23123349
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