Positively charged micelles based on a triblock copolymer demonstrate enhanced corneal penetration

Jingguo Li, Zhanrong Li, Tianyang Zhou, Junjie Zhang, Huiyun Xia, Heng Li, Jijun He, Siyu He, Liya Wang Henan Eye Institute, Henan Eye Hospital, Henan Provincial People’s Hospital and Zhengzhou University People’s Hospital, Zhengzhou, People’s Republic of Chin...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Li J, Li Z, Zhou T, Zhang J, Xia H, Li H, He J, He S, Wang L
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2015
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/bc269f190a03425d988cb26c434e25ad
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:bc269f190a03425d988cb26c434e25ad
record_format	dspace
spelling	oai:doaj.org-article:bc269f190a03425d988cb26c434e25ad2021-12-02T02:31:40ZPositively charged micelles based on a triblock copolymer demonstrate enhanced corneal penetration1178-2013https://doaj.org/article/bc269f190a03425d988cb26c434e25ad2015-09-01T00:00:00Zhttps://www.dovepress.com/positively-charged-micelles-based-on-a-triblock-copolymer-demonstrate--peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Jingguo Li, Zhanrong Li, Tianyang Zhou, Junjie Zhang, Huiyun Xia, Heng Li, Jijun He, Siyu He, Liya Wang Henan Eye Institute, Henan Eye Hospital, Henan Provincial People’s Hospital and Zhengzhou University People’s Hospital, Zhengzhou, People’s Republic of China Purpose: The cornea is a main barrier to drug penetration after topical application. The aim of this study was to evaluate the abilities of micelles generated from a positively charged triblock copolymer to penetrate the cornea after topical application. Methods: The triblock copolymer poly(ethylene glycol)-poly(ε-caprolactone)-g-polyethyleneimine was synthesized, and the physicochemical properties of the self-assembled polymeric micelles were investigated, including hydrodynamic size, zeta potential, morphology, drug-loading content, drug-loading efficiency, and in vitro drug release. Using fluorescein diacetate as a model drug, the penetration capabilities of the polymeric micelles were monitored in vivo using a two-photon scanning fluorescence microscopy on murine corneas after topical application. Results: The polymer was successfully synthesized and confirmed using nuclear magnetic resonance and Fourier transform infrared. The polymeric micelles had an average particle size of 28 nm, a zeta potential of approximately +12 mV, and a spherical morphology. The drug-loading efficiency and drug-loading content were 75.37% and 3.47%, respectively, which indicates that the polymeric micelles possess a high drug-loading capacity. The polymeric micelles also exhibited controlled-release behavior in vitro. Compared to the control, the positively charged polymeric micelles significantly penetrated through the cornea. Conclusion: Positively charged micelles generated from a triblock copolymer are a promising vehicle for the topical delivery of hydrophobic agents in ocular applications. Keywords: corneal barriers, polymeric micelles, topical administration, corneal penetration, controlled releaseLi JLi ZZhou TZhang JXia HLi HHe JHe SWang LDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2015, Iss default, Pp 6027-6037 (2015)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Li J Li Z Zhou T Zhang J Xia H Li H He J He S Wang L Positively charged micelles based on a triblock copolymer demonstrate enhanced corneal penetration
description	Jingguo Li, Zhanrong Li, Tianyang Zhou, Junjie Zhang, Huiyun Xia, Heng Li, Jijun He, Siyu He, Liya Wang Henan Eye Institute, Henan Eye Hospital, Henan Provincial People’s Hospital and Zhengzhou University People’s Hospital, Zhengzhou, People’s Republic of China Purpose: The cornea is a main barrier to drug penetration after topical application. The aim of this study was to evaluate the abilities of micelles generated from a positively charged triblock copolymer to penetrate the cornea after topical application. Methods: The triblock copolymer poly(ethylene glycol)-poly(ε-caprolactone)-g-polyethyleneimine was synthesized, and the physicochemical properties of the self-assembled polymeric micelles were investigated, including hydrodynamic size, zeta potential, morphology, drug-loading content, drug-loading efficiency, and in vitro drug release. Using fluorescein diacetate as a model drug, the penetration capabilities of the polymeric micelles were monitored in vivo using a two-photon scanning fluorescence microscopy on murine corneas after topical application. Results: The polymer was successfully synthesized and confirmed using nuclear magnetic resonance and Fourier transform infrared. The polymeric micelles had an average particle size of 28 nm, a zeta potential of approximately +12 mV, and a spherical morphology. The drug-loading efficiency and drug-loading content were 75.37% and 3.47%, respectively, which indicates that the polymeric micelles possess a high drug-loading capacity. The polymeric micelles also exhibited controlled-release behavior in vitro. Compared to the control, the positively charged polymeric micelles significantly penetrated through the cornea. Conclusion: Positively charged micelles generated from a triblock copolymer are a promising vehicle for the topical delivery of hydrophobic agents in ocular applications. Keywords: corneal barriers, polymeric micelles, topical administration, corneal penetration, controlled release
format	article
author	Li J Li Z Zhou T Zhang J Xia H Li H He J He S Wang L
author_facet	Li J Li Z Zhou T Zhang J Xia H Li H He J He S Wang L
author_sort	Li J
title	Positively charged micelles based on a triblock copolymer demonstrate enhanced corneal penetration
title_short	Positively charged micelles based on a triblock copolymer demonstrate enhanced corneal penetration
title_full	Positively charged micelles based on a triblock copolymer demonstrate enhanced corneal penetration
title_fullStr	Positively charged micelles based on a triblock copolymer demonstrate enhanced corneal penetration
title_full_unstemmed	Positively charged micelles based on a triblock copolymer demonstrate enhanced corneal penetration
title_sort	positively charged micelles based on a triblock copolymer demonstrate enhanced corneal penetration
publisher	Dove Medical Press
publishDate	2015
url	https://doaj.org/article/bc269f190a03425d988cb26c434e25ad
work_keys_str_mv	AT lij positivelychargedmicellesbasedonatriblockcopolymerdemonstrateenhancedcornealpenetration AT liz positivelychargedmicellesbasedonatriblockcopolymerdemonstrateenhancedcornealpenetration AT zhout positivelychargedmicellesbasedonatriblockcopolymerdemonstrateenhancedcornealpenetration AT zhangj positivelychargedmicellesbasedonatriblockcopolymerdemonstrateenhancedcornealpenetration AT xiah positivelychargedmicellesbasedonatriblockcopolymerdemonstrateenhancedcornealpenetration AT lih positivelychargedmicellesbasedonatriblockcopolymerdemonstrateenhancedcornealpenetration AT hej positivelychargedmicellesbasedonatriblockcopolymerdemonstrateenhancedcornealpenetration AT hes positivelychargedmicellesbasedonatriblockcopolymerdemonstrateenhancedcornealpenetration AT wangl positivelychargedmicellesbasedonatriblockcopolymerdemonstrateenhancedcornealpenetration
_version_	1718402435216572416

Positively charged micelles based on a triblock copolymer demonstrate enhanced corneal penetration

Ejemplares similares