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Published on: February 14, 2018
Essential Oil-Based Design and Development of Novel Anti-Candida Azoles Formulation
Rania Hamdy1,2, Bahgat Fayed1,3, Alshaimaa M Hamoda1,4
1Research Institute for Medical and Health Sciences, University of Sharjah, P.O. Box, Sharjah 27272, UAE.
Abstract:
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.
Insights
New azole compounds combat drug-resistant Candida infections, including the emergent Candida auris. Formulated nanoparticles offer prolonged activity and no toxicity, addressing urgent needs for effective antifungal therapies.
Area of Science:
- Mycology
- Medicinal Chemistry
- Nanotechnology
Background:
- Candida species, particularly Candida albicans and the emergent Candida auris, cause significant human infections with high mortality rates.
- Multidrug resistance in Candida species necessitates the development of novel antifungal agents effective against both established and emerging pathogens.
- Existing antifungal compounds primarily target Candida albicans, with limited options available for Candida auris.
Purpose of the Study:
- To design and synthesize novel azole-containing compounds inspired by cuminaldehyde and azole antifungals.
- To evaluate the anti-Candida activity of the synthesized compounds against Candida albicans and Candida auris.
- To develop and assess a nanoparticle formulation of the most potent compound for improved drug delivery and reduced toxicity.
Main Methods:
- Synthesis of a series of novel azole compounds (UoST1-11).
- In vitro antifungal activity testing against Candida albicans and Candida auris.
- Formulation of the lead compound (UoST5) into polymeric nanoparticles (NPs).
- Evaluation of UoST5-NPs for drug release kinetics, prolonged activity, and toxicity.
Main Results:
- The synthesized UoST compounds demonstrated significant antifungal activity against both Candida albicans and Candida auris.
- The lead compound, UoST5, when formulated into nanoparticles (UoST5-NPs), exhibited comparable efficacy to the free drug.
- UoST5-NPs showed a controlled release profile (25% in 24 h), prolonged antifungal activity up to 48 h, and no observed toxicity.
Conclusions:
- Novel azole compounds (UoST series) effectively target both Candida albicans and the emergent Candida auris.
- The nanoparticle formulation (UoST5-NPs) enhances antifungal efficacy with prolonged action and improved safety profile.
- These findings offer a promising strategy for developing new treatments against multidrug-resistant Candida infections.
