Enhanced antifungal activity of voriconazole-loaded nanostructured lipid carriers against Candida albicans with a dimorphic switching model

Baocheng Tian,1 Qi Yan,1 Juan Wang,1 Chen Ding,2 Sixiang Sai1 1School of Pharmacy, Binzhou Medical University, Yantai, 2College of Life and Health Science, Northeastern University, Shenyang, People’s Republic of China Abstract: Candida commonly adheres to implanted medical devices and fo...

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Autores principales: Tian B, Yan Q, Wang J, Ding C, Sai S
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Publicado: Dove Medical Press 2017
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spelling oai:doaj.org-article:c79b4bc83dab40deacf466668d552f6b2021-12-02T02:42:32ZEnhanced antifungal activity of voriconazole-loaded nanostructured lipid carriers against Candida albicans with a dimorphic switching model1178-2013https://doaj.org/article/c79b4bc83dab40deacf466668d552f6b2017-09-01T00:00:00Zhttps://www.dovepress.com/enhanced-antifungal-activity-of-voriconazole-loaded-nanostructured-lip-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Baocheng Tian,1 Qi Yan,1 Juan Wang,1 Chen Ding,2 Sixiang Sai1 1School of Pharmacy, Binzhou Medical University, Yantai, 2College of Life and Health Science, Northeastern University, Shenyang, People’s Republic of China Abstract: Candida commonly adheres to implanted medical devices and forms biofilms. Due to the minimal activity of current antifungals against biofilms, new drugs or drug-delivery systems to treat these persistent infections are urgently needed. In the present investigation, voriconazole-loaded nanostructured lipid carriers (Vrc-NLCs) were formulated for enhanced drug-delivery efficiency to C. albicans to increase the antifungal activity of Vrc and to improve the treatment of infectious Candida diseases. Vrc-NLCs were prepared by a hot-melt, high-pressure homogenization method, and size distribution, ζ-potential, morphology, drug-encapsulation efficiency, drug loading, and physical stability were characterized. The antifungal activity of Vrc-NLCs in vitro was tested during planktonic and biofilm growth in C. albicans. The mean particle size of the Vrc-NLCs was 45.62±0.53 nm, and they exhibited spheroid-like morphology, smooth surfaces, and ζ-potential of -0.69±0.03 mV. Encapsulation efficiency and drug loading of Vrc-NLCs were 75.37%±2.65% and 3.77%±0.13%, respectively. Physical stability results revealed that despite the low measured ζ-potential, the dispersion of the Vrc-NLCs was stable during their 3-week storage at 4°C. The minimum inhibitory concentration of Vrc-NLCs was identical to that of Vrc. However, the inhibition rate of Vrc-NLCs at lower concentrations was significantly higher than that of Vrc during planktonic growth in C. albicans in yeast-extract peptone dextrose medium. Surprisingly, Vrc-NLCs treatment reduced cell density in biofilm growth in C. albicans and induced more switches form hyphal cells to yeast cells compared with Vrc treatment. In conclusion, Vrc-NLCs maintain antifungal activity of Vrc and increase antifungal drug-delivery efficiency to C. albicans. Therefore, Vrc-NLCs will greatly contribute to the treatment of infectious diseases caused by C. albicans. Keywords: antifungal activity, Candida albicans, voriconazole, nanostructured lipid carriers, biofilmsTian BYan QWang JDing CSai SDove Medical Pressarticleantifungal activityCandida albicansvoriconazolenanostructured lipid carriersbiofilm.Medicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 12, Pp 7131-7141 (2017)
institution DOAJ
collection DOAJ
language EN
topic antifungal activity
Candida albicans
voriconazole
nanostructured lipid carriers
biofilm.
Medicine (General)
R5-920
spellingShingle antifungal activity
Candida albicans
voriconazole
nanostructured lipid carriers
biofilm.
Medicine (General)
R5-920
Tian B
Yan Q
Wang J
Ding C
Sai S
Enhanced antifungal activity of voriconazole-loaded nanostructured lipid carriers against Candida albicans with a dimorphic switching model
description Baocheng Tian,1 Qi Yan,1 Juan Wang,1 Chen Ding,2 Sixiang Sai1 1School of Pharmacy, Binzhou Medical University, Yantai, 2College of Life and Health Science, Northeastern University, Shenyang, People’s Republic of China Abstract: Candida commonly adheres to implanted medical devices and forms biofilms. Due to the minimal activity of current antifungals against biofilms, new drugs or drug-delivery systems to treat these persistent infections are urgently needed. In the present investigation, voriconazole-loaded nanostructured lipid carriers (Vrc-NLCs) were formulated for enhanced drug-delivery efficiency to C. albicans to increase the antifungal activity of Vrc and to improve the treatment of infectious Candida diseases. Vrc-NLCs were prepared by a hot-melt, high-pressure homogenization method, and size distribution, ζ-potential, morphology, drug-encapsulation efficiency, drug loading, and physical stability were characterized. The antifungal activity of Vrc-NLCs in vitro was tested during planktonic and biofilm growth in C. albicans. The mean particle size of the Vrc-NLCs was 45.62±0.53 nm, and they exhibited spheroid-like morphology, smooth surfaces, and ζ-potential of -0.69±0.03 mV. Encapsulation efficiency and drug loading of Vrc-NLCs were 75.37%±2.65% and 3.77%±0.13%, respectively. Physical stability results revealed that despite the low measured ζ-potential, the dispersion of the Vrc-NLCs was stable during their 3-week storage at 4°C. The minimum inhibitory concentration of Vrc-NLCs was identical to that of Vrc. However, the inhibition rate of Vrc-NLCs at lower concentrations was significantly higher than that of Vrc during planktonic growth in C. albicans in yeast-extract peptone dextrose medium. Surprisingly, Vrc-NLCs treatment reduced cell density in biofilm growth in C. albicans and induced more switches form hyphal cells to yeast cells compared with Vrc treatment. In conclusion, Vrc-NLCs maintain antifungal activity of Vrc and increase antifungal drug-delivery efficiency to C. albicans. Therefore, Vrc-NLCs will greatly contribute to the treatment of infectious diseases caused by C. albicans. Keywords: antifungal activity, Candida albicans, voriconazole, nanostructured lipid carriers, biofilms
format article
author Tian B
Yan Q
Wang J
Ding C
Sai S
author_facet Tian B
Yan Q
Wang J
Ding C
Sai S
author_sort Tian B
title Enhanced antifungal activity of voriconazole-loaded nanostructured lipid carriers against Candida albicans with a dimorphic switching model
title_short Enhanced antifungal activity of voriconazole-loaded nanostructured lipid carriers against Candida albicans with a dimorphic switching model
title_full Enhanced antifungal activity of voriconazole-loaded nanostructured lipid carriers against Candida albicans with a dimorphic switching model
title_fullStr Enhanced antifungal activity of voriconazole-loaded nanostructured lipid carriers against Candida albicans with a dimorphic switching model
title_full_unstemmed Enhanced antifungal activity of voriconazole-loaded nanostructured lipid carriers against Candida albicans with a dimorphic switching model
title_sort enhanced antifungal activity of voriconazole-loaded nanostructured lipid carriers against candida albicans with a dimorphic switching model
publisher Dove Medical Press
publishDate 2017
url https://doaj.org/article/c79b4bc83dab40deacf466668d552f6b
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