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Modified Clerodanes from the Essential Oil of Dodonea viscosa Leaves
Open AccessArticle

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

Research Institute for Medical and Health Sciences, University of Sharjah, P.O. Box, Sharjah 27272, UAE
Department of Medicinal Chemistry, Faculty of Pharmacy, Zagazig University, Zagazig 44519, Egypt
Chemistry of Natural and Microbial Product Department, National Research Centre, Cairo 12622, Egypt
Department of Pharmacognosy, Faculty of Pharmacy, Assiut University, Assiut 71515, Egypt
College of Pharmacy, University of Sharjah, P.O. Box, Sharjah 27272, UAE
Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt
Author to whom correspondence should be addressed.
Academic Editors: Valtcho Jeliazkov, Murray B. Isman, Farid Chemat, Vassya Bankova and Niko Radulović
Molecules 2020, 25(6), 1463;
Received: 29 February 2020 / Revised: 19 March 2020 / Accepted: 20 March 2020 / Published: 24 March 2020
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. View Full-Text
Keywords: Candida albicans; Candida auris; anti-fungal; nanoparticles; azoles; essential oil Candida albicans; Candida auris; anti-fungal; nanoparticles; azoles; essential oil
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Hamdy, R.; Fayed, B.; Hamoda, A.M.; Rawas-Qalaji, M.; Haider, M.; Soliman, S.S.M. Essential Oil-Based Design and Development of Novel Anti-Candida Azoles Formulation. Molecules 2020, 25, 1463.

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