Cargando…

Essential Oil-Based Design and Development of Novel Anti-Candida Azoles Formulation

Candida is the most common fungal class, causing both superficial and invasive diseases in humans. Although Candida albicans is the most common cause of fungal infections in humans, C. auris is a new emergent serious pathogen causing complications similar to those of C. albicans. Both C. albicans an...

Descripción completa

Detalles Bibliográficos
Autores principales: Hamdy, Rania, Fayed, Bahgat, Hamoda, Alshaimaa M., Rawas-Qalaji, Mutasem, Haider, Mohamed, Soliman, Sameh S. M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7146627/
https://www.ncbi.nlm.nih.gov/pubmed/32213931
http://dx.doi.org/10.3390/molecules25061463
_version_ 1783520244803829760
author Hamdy, Rania
Fayed, Bahgat
Hamoda, Alshaimaa M.
Rawas-Qalaji, Mutasem
Haider, Mohamed
Soliman, Sameh S. M.
author_facet Hamdy, Rania
Fayed, Bahgat
Hamoda, Alshaimaa M.
Rawas-Qalaji, Mutasem
Haider, Mohamed
Soliman, Sameh S. M.
author_sort Hamdy, Rania
collection PubMed
description Candida is the most common fungal class, causing both superficial and invasive diseases in humans. Although Candida albicans is the most common cause of fungal infections in humans, C. auris is a new emergent serious pathogen causing complications similar to those of C. albicans. Both C. albicans and C. auris are associated with high mortality rates, mainly because of their multidrug-resistance patterns against most available antifungal drugs. Although several compounds were designed against C. albicans, very few or none were tested on C. auris. Therefore, it is urgent to develop novel effective antifungal drugs that can accommodate not only C. albicans, but also other Candida spp., particularly newly emergent one, including C. auris. Inspired by the significant broad-spectrum antifungal activities of the essential oil cuminaldehyde and the reported wide incorporation of azoles in the antifungal drugs, a series of compounds (UoST1-11) was designed and developed. The new compounds were designed to overcome the toxicity of the aldehyde group of cuminaldehyde and benefit from the antifungal selectivity of azoles. The new developed UoST compounds showed significant anti-Candida activities against both Candida species. The best candidate compound, UoST5, was further formulated into polymeric nanoparticles (NPs). The new formula, UoST5-NPs, showed similar activities to the nanoparticles-free drug, while providing only 25% release after 24 h, maintainng prolonged activity up to 48 h and affording no toxicity. In conclusion, new azole formulations with significantly enhanced activities against C. albicans and C. auris, while maintaining prolonged action and no toxicities at lower concentrations, were developed.
format Online
Article
Text
id pubmed-7146627
institution National Center for Biotechnology Information
language English
publishDate 2020
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-71466272020-04-20 Essential Oil-Based Design and Development of Novel Anti-Candida Azoles Formulation Hamdy, Rania Fayed, Bahgat Hamoda, Alshaimaa M. Rawas-Qalaji, Mutasem Haider, Mohamed Soliman, Sameh S. M. Molecules Article Candida is the most common fungal class, causing both superficial and invasive diseases in humans. Although Candida albicans is the most common cause of fungal infections in humans, C. auris is a new emergent serious pathogen causing complications similar to those of C. albicans. Both C. albicans and C. auris are associated with high mortality rates, mainly because of their multidrug-resistance patterns against most available antifungal drugs. Although several compounds were designed against C. albicans, very few or none were tested on C. auris. Therefore, it is urgent to develop novel effective antifungal drugs that can accommodate not only C. albicans, but also other Candida spp., particularly newly emergent one, including C. auris. Inspired by the significant broad-spectrum antifungal activities of the essential oil cuminaldehyde and the reported wide incorporation of azoles in the antifungal drugs, a series of compounds (UoST1-11) was designed and developed. The new compounds were designed to overcome the toxicity of the aldehyde group of cuminaldehyde and benefit from the antifungal selectivity of azoles. The new developed UoST compounds showed significant anti-Candida activities against both Candida species. The best candidate compound, UoST5, was further formulated into polymeric nanoparticles (NPs). The new formula, UoST5-NPs, showed similar activities to the nanoparticles-free drug, while providing only 25% release after 24 h, maintainng prolonged activity up to 48 h and affording no toxicity. In conclusion, new azole formulations with significantly enhanced activities against C. albicans and C. auris, while maintaining prolonged action and no toxicities at lower concentrations, were developed. MDPI 2020-03-24 /pmc/articles/PMC7146627/ /pubmed/32213931 http://dx.doi.org/10.3390/molecules25061463 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
Hamdy, Rania
Fayed, Bahgat
Hamoda, Alshaimaa M.
Rawas-Qalaji, Mutasem
Haider, Mohamed
Soliman, Sameh S. M.
Essential Oil-Based Design and Development of Novel Anti-Candida Azoles Formulation
title Essential Oil-Based Design and Development of Novel Anti-Candida Azoles Formulation
title_full Essential Oil-Based Design and Development of Novel Anti-Candida Azoles Formulation
title_fullStr Essential Oil-Based Design and Development of Novel Anti-Candida Azoles Formulation
title_full_unstemmed Essential Oil-Based Design and Development of Novel Anti-Candida Azoles Formulation
title_short Essential Oil-Based Design and Development of Novel Anti-Candida Azoles Formulation
title_sort essential oil-based design and development of novel anti-candida azoles formulation
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7146627/
https://www.ncbi.nlm.nih.gov/pubmed/32213931
http://dx.doi.org/10.3390/molecules25061463
work_keys_str_mv AT hamdyrania essentialoilbaseddesignanddevelopmentofnovelanticandidaazolesformulation
AT fayedbahgat essentialoilbaseddesignanddevelopmentofnovelanticandidaazolesformulation
AT hamodaalshaimaam essentialoilbaseddesignanddevelopmentofnovelanticandidaazolesformulation
AT rawasqalajimutasem essentialoilbaseddesignanddevelopmentofnovelanticandidaazolesformulation
AT haidermohamed essentialoilbaseddesignanddevelopmentofnovelanticandidaazolesformulation
AT solimansamehsm essentialoilbaseddesignanddevelopmentofnovelanticandidaazolesformulation