Antifungal efficacy of itraconazole-loaded TPGS-b-(PCL-ran-PGA) nanoparticles

Lixin Qiu,1,2,* Bicheng Hu,1,4,* Hongbo Chen,2,3 Shanshan Li,5 Yuqian Hu,2,3 Yi Zheng,2,3 Xinxing Wu1 1Institute of Virology, School of Medicine, State Key Laboratory of Virology, Wuhan University, Wuhan, Hubei, People’s Republic of China; 2The Shenzhen Key Lab of Gene...

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Autores principales:	Qiu L, Hu B, Chen H, Li S, Hu Y, Zheng Y, Wu X
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2015
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/9e935b5fa9c346989fdde4bb618a37fe
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spelling	oai:doaj.org-article:9e935b5fa9c346989fdde4bb618a37fe2021-12-02T07:36:57ZAntifungal efficacy of itraconazole-loaded TPGS-b-(PCL-ran-PGA) nanoparticles1178-2013https://doaj.org/article/9e935b5fa9c346989fdde4bb618a37fe2015-02-01T00:00:00Zhttp://www.dovepress.com/antifungal-efficacy-of-itraconazole-loaded-tpgs-b-pcl-ran-pga-nanopart-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013 Lixin Qiu,1,2,* Bicheng Hu,1,4,* Hongbo Chen,2,3 Shanshan Li,5 Yuqian Hu,2,3 Yi Zheng,2,3 Xinxing Wu1 1Institute of Virology, School of Medicine, State Key Laboratory of Virology, Wuhan University, Wuhan, Hubei, People’s Republic of China; 2The Shenzhen Key Lab of Gene and Antibody Therapy, Center for Biotech and Biomedicine, Division of Life and Health Sciences, Graduate School at Shenzhen, Tsinghua University, Shenzhen, Guangdong, People’s Republic of China; 3School of Life Sciences, Tsinghua University, Beijing, People’s Republic of China; 4The Clinical Laboratory, Wuhan No 1 Hospital, Wuhan, Hubei, People’s Republic of China; 5Department of Plant Pathology and Microbiology, Iowa State University, Ames, IA, USA *These authors contributed equally to this work Abstract: This research was conducted to formulate biodegradable itraconazole (ITZ)-loaded d-a-tocopheryl polyethylene glycol 1000 succinate-b-poly(e-caprolactone-ran-glycolide) (TPGS-b-(PCL-ran-PGA); TPP) nanoparticles (NPs) (designed as ITZ-loaded TPP NPs) to improve antifungal efficacy. ITZ-loaded TPP NPs were prepared by a modified double-emulsion method, and their size distribution, morphology, zeta potential, drug encapsulation efficiency, drug-release profile, and antifungal effects were characterized. The cytotoxicity of ITZ-loaded-TPP NPs on HeLa cells and fibroblasts was measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide (MTT) method. The in vivo antifungal activity of ITZ-loaded-TPP NPs was examined in mice by administrating 5×105 colony forming units of Candida albicans through the tail vein. The survival rate and survival time of the mice was observed. The fungal count and pathology of lung tissue was analyzed. The data showed that ITZ-loaded-TPP NPs have size of 265±5.8 nm, zeta potential of -31±0.5 mV, high encapsulation efficiency (95%), and extended drug-release profile. ITZ-loaded-TPP NPs at a high concentration of 25 mg/mL had no cytotoxicity on HeLa cells and fibroblasts. Furthermore, ITZ-loaded-TPP NPs achieved a higher level of antifungal activity both in vitro and in vivo. The survival rate and duration was higher in mice treated by ITZ-loaded-TPP NPs than in the other groups (P<0.05). In conclusion, ITZ-loaded-TPP NPs significantly improved ITZ bioavailability by increasing its aqueous dispersibility and extending the duration of drug release, thereby improving the antifungal efficacy of the ITZ agent. Keywords: antifungal, Candida albicans, itraconazole (ITZ), nanoparticles (NPs), TPGS-b-(PCL-ran-PGA) (TPP)Qiu LHu BChen HLi SHu YZheng YWu XDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2015, Iss default, Pp 1415-1423 (2015)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Qiu L Hu B Chen H Li S Hu Y Zheng Y Wu X Antifungal efficacy of itraconazole-loaded TPGS-b-(PCL-ran-PGA) nanoparticles
description	Lixin Qiu,1,2,* Bicheng Hu,1,4,* Hongbo Chen,2,3 Shanshan Li,5 Yuqian Hu,2,3 Yi Zheng,2,3 Xinxing Wu1 1Institute of Virology, School of Medicine, State Key Laboratory of Virology, Wuhan University, Wuhan, Hubei, People’s Republic of China; 2The Shenzhen Key Lab of Gene and Antibody Therapy, Center for Biotech and Biomedicine, Division of Life and Health Sciences, Graduate School at Shenzhen, Tsinghua University, Shenzhen, Guangdong, People’s Republic of China; 3School of Life Sciences, Tsinghua University, Beijing, People’s Republic of China; 4The Clinical Laboratory, Wuhan No 1 Hospital, Wuhan, Hubei, People’s Republic of China; 5Department of Plant Pathology and Microbiology, Iowa State University, Ames, IA, USA *These authors contributed equally to this work Abstract: This research was conducted to formulate biodegradable itraconazole (ITZ)-loaded d-a-tocopheryl polyethylene glycol 1000 succinate-b-poly(e-caprolactone-ran-glycolide) (TPGS-b-(PCL-ran-PGA); TPP) nanoparticles (NPs) (designed as ITZ-loaded TPP NPs) to improve antifungal efficacy. ITZ-loaded TPP NPs were prepared by a modified double-emulsion method, and their size distribution, morphology, zeta potential, drug encapsulation efficiency, drug-release profile, and antifungal effects were characterized. The cytotoxicity of ITZ-loaded-TPP NPs on HeLa cells and fibroblasts was measured using the 3-(4,5-dimethylthiazol-2-yl)-2,5- diphenyltetrazolium bromide (MTT) method. The in vivo antifungal activity of ITZ-loaded-TPP NPs was examined in mice by administrating 5×105 colony forming units of Candida albicans through the tail vein. The survival rate and survival time of the mice was observed. The fungal count and pathology of lung tissue was analyzed. The data showed that ITZ-loaded-TPP NPs have size of 265±5.8 nm, zeta potential of -31±0.5 mV, high encapsulation efficiency (95%), and extended drug-release profile. ITZ-loaded-TPP NPs at a high concentration of 25 mg/mL had no cytotoxicity on HeLa cells and fibroblasts. Furthermore, ITZ-loaded-TPP NPs achieved a higher level of antifungal activity both in vitro and in vivo. The survival rate and duration was higher in mice treated by ITZ-loaded-TPP NPs than in the other groups (P<0.05). In conclusion, ITZ-loaded-TPP NPs significantly improved ITZ bioavailability by increasing its aqueous dispersibility and extending the duration of drug release, thereby improving the antifungal efficacy of the ITZ agent. Keywords: antifungal, Candida albicans, itraconazole (ITZ), nanoparticles (NPs), TPGS-b-(PCL-ran-PGA) (TPP)
format	article
author	Qiu L Hu B Chen H Li S Hu Y Zheng Y Wu X
author_facet	Qiu L Hu B Chen H Li S Hu Y Zheng Y Wu X
author_sort	Qiu L
title	Antifungal efficacy of itraconazole-loaded TPGS-b-(PCL-ran-PGA) nanoparticles
title_short	Antifungal efficacy of itraconazole-loaded TPGS-b-(PCL-ran-PGA) nanoparticles
title_full	Antifungal efficacy of itraconazole-loaded TPGS-b-(PCL-ran-PGA) nanoparticles
title_fullStr	Antifungal efficacy of itraconazole-loaded TPGS-b-(PCL-ran-PGA) nanoparticles
title_full_unstemmed	Antifungal efficacy of itraconazole-loaded TPGS-b-(PCL-ran-PGA) nanoparticles
title_sort	antifungal efficacy of itraconazole-loaded tpgs-b-(pcl-ran-pga) nanoparticles
publisher	Dove Medical Press
publishDate	2015
url	https://doaj.org/article/9e935b5fa9c346989fdde4bb618a37fe
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Antifungal efficacy of itraconazole-loaded TPGS-b-(PCL-ran-PGA) nanoparticles

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