Assessment to the Antifungal Effects in vitro and the Ocular Pharmacokinetics of Solid-Lipid Nanoparticle in Rabbits

Zhen Liang, Zhen Zhang, Jingjing Yang, Ping Lu, Tianyang Zhou, Jingguo Li, Junjie Zhang Henan Eye Hospital, Henan Provincial People’s Hospital & People’s Hospital of Zhengzhou University, Zhengzhou, People’s Republic of ChinaCorrespondence: Jingguo Li; Junjie ZhangHenan Eye Hospital, Henan Provi...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Liang Z, Zhang Z, Yang J, Lu P, Zhou T, Li J, Zhang J
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2021
Materias:	fungal keratitis solid-lipid nanoparticles econazole topical administration corneal penetration Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/b7a82e2672cd46eda897e60a713dfb7c
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:b7a82e2672cd46eda897e60a713dfb7c
record_format	dspace
spelling	oai:doaj.org-article:b7a82e2672cd46eda897e60a713dfb7c2021-12-02T18:56:23ZAssessment to the Antifungal Effects in vitro and the Ocular Pharmacokinetics of Solid-Lipid Nanoparticle in Rabbits1178-2013https://doaj.org/article/b7a82e2672cd46eda897e60a713dfb7c2021-11-01T00:00:00Zhttps://www.dovepress.com/assessment-to-the-antifungal-effects-in-vitro-and-the-ocular-pharmacok-peer-reviewed-fulltext-article-IJNhttps://doaj.org/toc/1178-2013Zhen Liang, Zhen Zhang, Jingjing Yang, Ping Lu, Tianyang Zhou, Jingguo Li, Junjie Zhang Henan Eye Hospital, Henan Provincial People’s Hospital & People’s Hospital of Zhengzhou University, Zhengzhou, People’s Republic of ChinaCorrespondence: Jingguo Li; Junjie ZhangHenan Eye Hospital, Henan Provincial People’s Hospital & People’s Hospital of Zhengzhou University, Number 7 Weiwu Road, Zhengzhou, People’s Republic of ChinaEmail lijingguo@zzu.edu.cn; zhangjunjie@zzu.edu.cnIntroduction: Fungal keratitis (FK) remains a severe sight-threatening disease, and case management is difficult due to ocular intrinsic barriers and drug shortages. Econazole (ECZ), a broad-spectrum antifungal agent, is limited in ocular applications due to the poor water solubility and strong irritant property.Methods: We successfully prepared solid-lipid nanoparticle-based ECZ eye drops (E-SLNs) by microemulsion method, and the physicochemical properties of E-SLNs were investigated. Corneal permeability, antifungal ability against Fusarium spp., irritation and bioavailability compared to ECZ Suspension (E-Susp) were evaluated in vitro and in vivo.Results: E-SLNs were a uniform and stable system which had an average particle size of 19 nm and a spherical morphology. E-SLNs also exhibited controlled release, enhanced antifungal activity without irritation. The pharmacokinetic analysis in vivo confirmed that E-SLNs showed an improved ocular bioavailability and the drug concentration in the cornea were above minimum inhibitory concentration (MIC) for 3 h after single administration.Conclusion: The E-SLNs colloid system is a promising therapeutic approach for fungal keratitis and could serve as a candidate strategy for other ocular diseases.Keywords: fungal keratitis, solid-lipid nanoparticles, econazole, topical administration, corneal penetrationLiang ZZhang ZYang JLu PZhou TLi JZhang JDove Medical Pressarticlefungal keratitissolid-lipid nanoparticleseconazoletopical administrationcorneal penetrationMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 16, Pp 7847-7857 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	fungal keratitis solid-lipid nanoparticles econazole topical administration corneal penetration Medicine (General) R5-920
spellingShingle	fungal keratitis solid-lipid nanoparticles econazole topical administration corneal penetration Medicine (General) R5-920 Liang Z Zhang Z Yang J Lu P Zhou T Li J Zhang J Assessment to the Antifungal Effects in vitro and the Ocular Pharmacokinetics of Solid-Lipid Nanoparticle in Rabbits
description	Zhen Liang, Zhen Zhang, Jingjing Yang, Ping Lu, Tianyang Zhou, Jingguo Li, Junjie Zhang Henan Eye Hospital, Henan Provincial People’s Hospital & People’s Hospital of Zhengzhou University, Zhengzhou, People’s Republic of ChinaCorrespondence: Jingguo Li; Junjie ZhangHenan Eye Hospital, Henan Provincial People’s Hospital & People’s Hospital of Zhengzhou University, Number 7 Weiwu Road, Zhengzhou, People’s Republic of ChinaEmail lijingguo@zzu.edu.cn; zhangjunjie@zzu.edu.cnIntroduction: Fungal keratitis (FK) remains a severe sight-threatening disease, and case management is difficult due to ocular intrinsic barriers and drug shortages. Econazole (ECZ), a broad-spectrum antifungal agent, is limited in ocular applications due to the poor water solubility and strong irritant property.Methods: We successfully prepared solid-lipid nanoparticle-based ECZ eye drops (E-SLNs) by microemulsion method, and the physicochemical properties of E-SLNs were investigated. Corneal permeability, antifungal ability against Fusarium spp., irritation and bioavailability compared to ECZ Suspension (E-Susp) were evaluated in vitro and in vivo.Results: E-SLNs were a uniform and stable system which had an average particle size of 19 nm and a spherical morphology. E-SLNs also exhibited controlled release, enhanced antifungal activity without irritation. The pharmacokinetic analysis in vivo confirmed that E-SLNs showed an improved ocular bioavailability and the drug concentration in the cornea were above minimum inhibitory concentration (MIC) for 3 h after single administration.Conclusion: The E-SLNs colloid system is a promising therapeutic approach for fungal keratitis and could serve as a candidate strategy for other ocular diseases.Keywords: fungal keratitis, solid-lipid nanoparticles, econazole, topical administration, corneal penetration
format	article
author	Liang Z Zhang Z Yang J Lu P Zhou T Li J Zhang J
author_facet	Liang Z Zhang Z Yang J Lu P Zhou T Li J Zhang J
author_sort	Liang Z
title	Assessment to the Antifungal Effects in vitro and the Ocular Pharmacokinetics of Solid-Lipid Nanoparticle in Rabbits
title_short	Assessment to the Antifungal Effects in vitro and the Ocular Pharmacokinetics of Solid-Lipid Nanoparticle in Rabbits
title_full	Assessment to the Antifungal Effects in vitro and the Ocular Pharmacokinetics of Solid-Lipid Nanoparticle in Rabbits
title_fullStr	Assessment to the Antifungal Effects in vitro and the Ocular Pharmacokinetics of Solid-Lipid Nanoparticle in Rabbits
title_full_unstemmed	Assessment to the Antifungal Effects in vitro and the Ocular Pharmacokinetics of Solid-Lipid Nanoparticle in Rabbits
title_sort	assessment to the antifungal effects in vitro and the ocular pharmacokinetics of solid-lipid nanoparticle in rabbits
publisher	Dove Medical Press
publishDate	2021
url	https://doaj.org/article/b7a82e2672cd46eda897e60a713dfb7c
work_keys_str_mv	AT liangz assessmenttotheantifungaleffectsinvitroandtheocularpharmacokineticsofsolidlipidnanoparticleinrabbits AT zhangz assessmenttotheantifungaleffectsinvitroandtheocularpharmacokineticsofsolidlipidnanoparticleinrabbits AT yangj assessmenttotheantifungaleffectsinvitroandtheocularpharmacokineticsofsolidlipidnanoparticleinrabbits AT lup assessmenttotheantifungaleffectsinvitroandtheocularpharmacokineticsofsolidlipidnanoparticleinrabbits AT zhout assessmenttotheantifungaleffectsinvitroandtheocularpharmacokineticsofsolidlipidnanoparticleinrabbits AT lij assessmenttotheantifungaleffectsinvitroandtheocularpharmacokineticsofsolidlipidnanoparticleinrabbits AT zhangj assessmenttotheantifungaleffectsinvitroandtheocularpharmacokineticsofsolidlipidnanoparticleinrabbits
_version_	1718377290349412352

Assessment to the Antifungal Effects in vitro and the Ocular Pharmacokinetics of Solid-Lipid Nanoparticle in Rabbits

Ejemplares similares