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Nano-Vesicle Based Anti-Fungal Formulation Shows Higher Stability, Skin Diffusion, Biosafety and Anti-Fungal Efficacy In Vitro

Opportunistic fungal infections are responsible for over 1.5 million deaths per year. This has created a need for highly effective antifungal medication to be as potent as possible. In this study, we improved the efficacy of a common over the counter (OTC) antifungal skin medication, miconazole, by...

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Autores principales: Deaguero, Isaac G., Huda, Md Nurul, Rodriguez, Victor, Zicari, Jade, Al-Hilal, Taslim A., Badruddoza, Abu Zayed Md, Nurunnabi, Md
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7355414/
https://www.ncbi.nlm.nih.gov/pubmed/32517047
http://dx.doi.org/10.3390/pharmaceutics12060516
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author Deaguero, Isaac G.
Huda, Md Nurul
Rodriguez, Victor
Zicari, Jade
Al-Hilal, Taslim A.
Badruddoza, Abu Zayed Md
Nurunnabi, Md
author_facet Deaguero, Isaac G.
Huda, Md Nurul
Rodriguez, Victor
Zicari, Jade
Al-Hilal, Taslim A.
Badruddoza, Abu Zayed Md
Nurunnabi, Md
author_sort Deaguero, Isaac G.
collection PubMed
description Opportunistic fungal infections are responsible for over 1.5 million deaths per year. This has created a need for highly effective antifungal medication to be as potent as possible. In this study, we improved the efficacy of a common over the counter (OTC) antifungal skin medication, miconazole, by encapsulating nano-molecules of the drug in cholesterol/sodium oleate nano-vesicles. These nano-vesicles were characterized to optimize their size, zeta potential, polydispersity index and encapsulation efficiency. Furthermore, these nano-vesicles were compared to a conventional miconazole-based commercially available cream to determine potential improvements via permeation through the stratum corneum, cytotoxicity, and antifungal capabilities. Our results found that the vesicle size was within the nano range (~300 nm), with moderate polydispersity and stability. When compared with the commercially available cream, Actavis, as well as free miconazole, the miconazole nano-vesicle formulation displayed enhanced fungal inhibition by a factor of three or more when compared to free miconazole. Furthermore, with smaller nanoparticle (NP) sizes, higher percentages of miconazole may be delivered, further enhancing the efficacy of miconazole’s antifungal capability. Cytotoxicity studies conducted with human dermal fibroblast cells confirm its biosafety and biocompatibility, as cell survival rate was observed to be twofold higher in nano-vesicle formulation than free miconazole. This formulation has the potential to treat fungal infections through increasing the retention time in the skin, improving the treatment approach, and by enhancing the efficacy via the use of nano-vesicles.
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spelling pubmed-73554142020-07-23 Nano-Vesicle Based Anti-Fungal Formulation Shows Higher Stability, Skin Diffusion, Biosafety and Anti-Fungal Efficacy In Vitro Deaguero, Isaac G. Huda, Md Nurul Rodriguez, Victor Zicari, Jade Al-Hilal, Taslim A. Badruddoza, Abu Zayed Md Nurunnabi, Md Pharmaceutics Article Opportunistic fungal infections are responsible for over 1.5 million deaths per year. This has created a need for highly effective antifungal medication to be as potent as possible. In this study, we improved the efficacy of a common over the counter (OTC) antifungal skin medication, miconazole, by encapsulating nano-molecules of the drug in cholesterol/sodium oleate nano-vesicles. These nano-vesicles were characterized to optimize their size, zeta potential, polydispersity index and encapsulation efficiency. Furthermore, these nano-vesicles were compared to a conventional miconazole-based commercially available cream to determine potential improvements via permeation through the stratum corneum, cytotoxicity, and antifungal capabilities. Our results found that the vesicle size was within the nano range (~300 nm), with moderate polydispersity and stability. When compared with the commercially available cream, Actavis, as well as free miconazole, the miconazole nano-vesicle formulation displayed enhanced fungal inhibition by a factor of three or more when compared to free miconazole. Furthermore, with smaller nanoparticle (NP) sizes, higher percentages of miconazole may be delivered, further enhancing the efficacy of miconazole’s antifungal capability. Cytotoxicity studies conducted with human dermal fibroblast cells confirm its biosafety and biocompatibility, as cell survival rate was observed to be twofold higher in nano-vesicle formulation than free miconazole. This formulation has the potential to treat fungal infections through increasing the retention time in the skin, improving the treatment approach, and by enhancing the efficacy via the use of nano-vesicles. MDPI 2020-06-05 /pmc/articles/PMC7355414/ /pubmed/32517047 http://dx.doi.org/10.3390/pharmaceutics12060516 Text en © 2020 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
Deaguero, Isaac G.
Huda, Md Nurul
Rodriguez, Victor
Zicari, Jade
Al-Hilal, Taslim A.
Badruddoza, Abu Zayed Md
Nurunnabi, Md
Nano-Vesicle Based Anti-Fungal Formulation Shows Higher Stability, Skin Diffusion, Biosafety and Anti-Fungal Efficacy In Vitro
title Nano-Vesicle Based Anti-Fungal Formulation Shows Higher Stability, Skin Diffusion, Biosafety and Anti-Fungal Efficacy In Vitro
title_full Nano-Vesicle Based Anti-Fungal Formulation Shows Higher Stability, Skin Diffusion, Biosafety and Anti-Fungal Efficacy In Vitro
title_fullStr Nano-Vesicle Based Anti-Fungal Formulation Shows Higher Stability, Skin Diffusion, Biosafety and Anti-Fungal Efficacy In Vitro
title_full_unstemmed Nano-Vesicle Based Anti-Fungal Formulation Shows Higher Stability, Skin Diffusion, Biosafety and Anti-Fungal Efficacy In Vitro
title_short Nano-Vesicle Based Anti-Fungal Formulation Shows Higher Stability, Skin Diffusion, Biosafety and Anti-Fungal Efficacy In Vitro
title_sort nano-vesicle based anti-fungal formulation shows higher stability, skin diffusion, biosafety and anti-fungal efficacy in vitro
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7355414/
https://www.ncbi.nlm.nih.gov/pubmed/32517047
http://dx.doi.org/10.3390/pharmaceutics12060516
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