Development of terbinafine solid lipid nanoparticles as a topical delivery system

Ying-Chen Chen,1* Der-Zen Liu,2* Jun-Jen Liu,3 Tsung-Wei Chang,1 Hsiu-O Ho,1 Ming-Thau Sheu,1,4 1School of Pharmacy, College of Pharmacy, 2Graduate Institute of Biomedical Materials and Engineering, 3School of Medical Laboratory Science and Biotechnology, 4Clinical Research Center and Traditional He...

Descripción completa

Guardado en:

Detalles Bibliográficos
Autores principales:	Chen Y-C, Liu D-Z, Liu J-J, Chang T-W, Ho H-O, Sheu M-T
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2012
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/f6e53fb3f6b340878713965aebca7e8c
Etiquetas:	Agregar Etiqueta Sin Etiquetas, Sea el primero en etiquetar este registro!

id	oai:doaj.org-article:f6e53fb3f6b340878713965aebca7e8c
record_format	dspace
spelling	oai:doaj.org-article:f6e53fb3f6b340878713965aebca7e8c2021-12-02T07:35:21ZDevelopment of terbinafine solid lipid nanoparticles as a topical delivery system1176-91141178-2013https://doaj.org/article/f6e53fb3f6b340878713965aebca7e8c2012-08-01T00:00:00Zhttp://www.dovepress.com/development-of-terbinafine-solid-lipid-nanoparticles-as-a-topical-deli-a10706https://doaj.org/toc/1176-9114https://doaj.org/toc/1178-2013Ying-Chen Chen,1* Der-Zen Liu,2* Jun-Jen Liu,3 Tsung-Wei Chang,1 Hsiu-O Ho,1 Ming-Thau Sheu,1,4 1School of Pharmacy, College of Pharmacy, 2Graduate Institute of Biomedical Materials and Engineering, 3School of Medical Laboratory Science and Biotechnology, 4Clinical Research Center and Traditional Herbal Medicine Research Center, Taipei Medical University Hospital, Taipei, Taiwan*Ying-Chen Chen and Der-Zen Liu contributed equally in the preparation of this manuscript.Abstract: To resolve problems of long treatment durations and frequent administration of the antifungal agent terbinafine (TB), solid lipid nanoparticles (SLNs) with the ability to load lipophilic drugs and nanosize were developed. The SLNs were manufactured by a microemulsion technique in which glyceryl monostearate (GMS), glyceryl behenate (Compritol&reg; 888; Gattefoss&eacute;), and glyceryl palmitostearate (Precirol&reg; ATO 5; Gattefoss&eacute;) were used as the solid lipid phases, Tween&reg; and Cremophor&reg; series as the surfactants, and propylene glycol as the cosurfactant to construct ternary phase diagrams. The skin of nude mice was used as a barrier membrane, and penetration levels of TB of the designed formulations and a commercial product, Lamisil&reg; OnceTM (Novartis Pharmaceuticals), in the stratum corneum (SC), viable epidermis, and dermis were measured; particle sizes were determined as an indicator of stability. The optimal SLN system contained a &lt;5% lipid phase and &gt;50% water phase. The addition of ethanol or etchants had no significant effect on enhancing the amount of TB that penetrated the skin layers, but it was enhanced by increasing the percentage of the lipid phase. Furthermore, the combination of GMS and Compritol&reg; 888 was able to increase the stable amount of TB that penetrated all skin layers. For the ACP1-GM1 (4% lipid phase; Compritol&reg; 888: GMS of 1:1) formulation, the amount of TB that penetrated the SC was similar to that of Lamisil&reg; OnceTM, whereas the amount of TB of the dermis was higher than that of Lamisil&reg; OnceTM at 12 hours, and it was almost the same as that of Lamisil&reg; OnceTM at 24 hours. It was concluded that the application of ACP1-GM1 for 12 hours might have an efficacy comparable to that of Lamisil&reg; OnceTM for 24 hours, which would resolve the practical problem of the longer administration period that is necessary for Lamisil&reg; OnceTM.Keywords: terbinafine, solid lipid nanoparticle, topical delivery systemChen Y-CLiu D-ZLiu J-JChang T-WHo H-OSheu M-TDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2012, Iss default, Pp 4409-4418 (2012)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 Chen Y-C Liu D-Z Liu J-J Chang T-W Ho H-O Sheu M-T Development of terbinafine solid lipid nanoparticles as a topical delivery system
description	Ying-Chen Chen,1* Der-Zen Liu,2* Jun-Jen Liu,3 Tsung-Wei Chang,1 Hsiu-O Ho,1 Ming-Thau Sheu,1,4 1School of Pharmacy, College of Pharmacy, 2Graduate Institute of Biomedical Materials and Engineering, 3School of Medical Laboratory Science and Biotechnology, 4Clinical Research Center and Traditional Herbal Medicine Research Center, Taipei Medical University Hospital, Taipei, Taiwan*Ying-Chen Chen and Der-Zen Liu contributed equally in the preparation of this manuscript.Abstract: To resolve problems of long treatment durations and frequent administration of the antifungal agent terbinafine (TB), solid lipid nanoparticles (SLNs) with the ability to load lipophilic drugs and nanosize were developed. The SLNs were manufactured by a microemulsion technique in which glyceryl monostearate (GMS), glyceryl behenate (Compritol&reg; 888; Gattefoss&eacute;), and glyceryl palmitostearate (Precirol&reg; ATO 5; Gattefoss&eacute;) were used as the solid lipid phases, Tween&reg; and Cremophor&reg; series as the surfactants, and propylene glycol as the cosurfactant to construct ternary phase diagrams. The skin of nude mice was used as a barrier membrane, and penetration levels of TB of the designed formulations and a commercial product, Lamisil&reg; OnceTM (Novartis Pharmaceuticals), in the stratum corneum (SC), viable epidermis, and dermis were measured; particle sizes were determined as an indicator of stability. The optimal SLN system contained a &lt;5% lipid phase and &gt;50% water phase. The addition of ethanol or etchants had no significant effect on enhancing the amount of TB that penetrated the skin layers, but it was enhanced by increasing the percentage of the lipid phase. Furthermore, the combination of GMS and Compritol&reg; 888 was able to increase the stable amount of TB that penetrated all skin layers. For the ACP1-GM1 (4% lipid phase; Compritol&reg; 888: GMS of 1:1) formulation, the amount of TB that penetrated the SC was similar to that of Lamisil&reg; OnceTM, whereas the amount of TB of the dermis was higher than that of Lamisil&reg; OnceTM at 12 hours, and it was almost the same as that of Lamisil&reg; OnceTM at 24 hours. It was concluded that the application of ACP1-GM1 for 12 hours might have an efficacy comparable to that of Lamisil&reg; OnceTM for 24 hours, which would resolve the practical problem of the longer administration period that is necessary for Lamisil&reg; OnceTM.Keywords: terbinafine, solid lipid nanoparticle, topical delivery system
format	article
author	Chen Y-C Liu D-Z Liu J-J Chang T-W Ho H-O Sheu M-T
author_facet	Chen Y-C Liu D-Z Liu J-J Chang T-W Ho H-O Sheu M-T
author_sort	Chen Y-C
title	Development of terbinafine solid lipid nanoparticles as a topical delivery system
title_short	Development of terbinafine solid lipid nanoparticles as a topical delivery system
title_full	Development of terbinafine solid lipid nanoparticles as a topical delivery system
title_fullStr	Development of terbinafine solid lipid nanoparticles as a topical delivery system
title_full_unstemmed	Development of terbinafine solid lipid nanoparticles as a topical delivery system
title_sort	development of terbinafine solid lipid nanoparticles as a topical delivery system
publisher	Dove Medical Press
publishDate	2012
url	https://doaj.org/article/f6e53fb3f6b340878713965aebca7e8c
work_keys_str_mv	AT chenyc developmentofterbinafinesolidlipidnanoparticlesasatopicaldeliverysystem AT liudz developmentofterbinafinesolidlipidnanoparticlesasatopicaldeliverysystem AT liujj developmentofterbinafinesolidlipidnanoparticlesasatopicaldeliverysystem AT changtw developmentofterbinafinesolidlipidnanoparticlesasatopicaldeliverysystem AT hoho developmentofterbinafinesolidlipidnanoparticlesasatopicaldeliverysystem AT sheumt developmentofterbinafinesolidlipidnanoparticlesasatopicaldeliverysystem
_version_	1718399376410279936

Development of terbinafine solid lipid nanoparticles as a topical delivery system

Ejemplares similares