Development and evaluation of nanostructured lipid carrier-based hydrogel for topical delivery of 5-fluorouracil

Paruvathanahalli Siddalingam Rajinikanth,1,2 Jestin Chellian2 1School of Pharmacy, Taylors University, 2School of Pharmacy, International Medical University, Kuala Lumpur, Malaysia Abstract: The aim of this study was to develop a nanostructured lipid carrier (NLC)-based hydrogel and study...

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Autores principales:	Rajinikanth PS, Chellian J
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2016
Materias:	Nanostructure lipid carrier Topical delivery Controlled release 5-Fluoruracil Skin Penetration Skin infection Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/723e6184da98422b8ef93c6cedba87ef
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spelling	oai:doaj.org-article:723e6184da98422b8ef93c6cedba87ef2021-12-02T03:58:40ZDevelopment and evaluation of nanostructured lipid carrier-based hydrogel for topical delivery of 5-fluorouracil1178-2013https://doaj.org/article/723e6184da98422b8ef93c6cedba87ef2016-10-01T00:00:00Zhttps://www.dovepress.com/development-and-evaluation-of-nanostructured-lipid-carrier-based-hydro-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Paruvathanahalli Siddalingam Rajinikanth,1,2 Jestin Chellian2 1School of Pharmacy, Taylors University, 2School of Pharmacy, International Medical University, Kuala Lumpur, Malaysia Abstract: The aim of this study was to develop a nanostructured lipid carrier (NLC)-based hydrogel and study its potential for the topical delivery of 5-fluorouracil (5-FU). Precirol® ATO 5 (glyceryl palmitostearate) and Labrasol® were selected as the solid and liquid lipid phases, respectively. Poloxamer 188 and Solutol® HS15 (polyoxyl-15-hydroxystearate) were selected as surfactants. The developed lipid formulations were dispersed in 1% Carbopol® 934 (poly[acrylic acid]) gel medium in order to maintain the topical application consistency. The average size, zeta potential, and polydispersity index for the 5-FU-NLC were found to be 208.32±8.21 nm, -21.82±0.40 mV, and 0.352±0.060, respectively. Transmission electron microscopy study revealed that 5-FU-NLC was <200 nm in size, with a spherical shape. In vitro drug permeation studies showed a release pattern with initial burst followed by sustained release, and the rate of 5-FU permeation was significantly improved for 5-FU-NLC gel (10.27±1.82 µg/cm2/h) as compared with plain 5-FU gel (2.85±1.12 µg/cm2/h). Further, skin retention studies showed a significant retention of 5-FU from the NLC gel (91.256±4.56 µg/cm2) as compared with that from the 5-FU plain gel (12.23±3.86 µg/cm2) in the rat skin. Skin irritation was also significantly reduced with 5-FU-NLC gel as compared with 5-FU plain gel. These results show that the prepared 5-FU-loaded NLC has high potential to improve the penetration of 5-FU through the stratum corneum, with enormous retention and with minimal skin irritation, which is the prerequisite for topically applied formulations. Keywords: nanostructured lipid carrier, topical delivery, controlled release, 5-fluorouracil, skin penetration, skin infectionRajinikanth PSChellian JDove Medical PressarticleNanostructure lipid carrierTopical deliveryControlled release5-FluoruracilSkin PenetrationSkin infectionMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 11, Pp 5067-5077 (2016)
institution	DOAJ
collection	DOAJ
language	EN
topic	Nanostructure lipid carrier Topical delivery Controlled release 5-Fluoruracil Skin Penetration Skin infection Medicine (General) R5-920
spellingShingle	Nanostructure lipid carrier Topical delivery Controlled release 5-Fluoruracil Skin Penetration Skin infection Medicine (General) R5-920 Rajinikanth PS Chellian J Development and evaluation of nanostructured lipid carrier-based hydrogel for topical delivery of 5-fluorouracil
description	Paruvathanahalli Siddalingam Rajinikanth,1,2 Jestin Chellian2 1School of Pharmacy, Taylors University, 2School of Pharmacy, International Medical University, Kuala Lumpur, Malaysia Abstract: The aim of this study was to develop a nanostructured lipid carrier (NLC)-based hydrogel and study its potential for the topical delivery of 5-fluorouracil (5-FU). Precirol® ATO 5 (glyceryl palmitostearate) and Labrasol® were selected as the solid and liquid lipid phases, respectively. Poloxamer 188 and Solutol® HS15 (polyoxyl-15-hydroxystearate) were selected as surfactants. The developed lipid formulations were dispersed in 1% Carbopol® 934 (poly[acrylic acid]) gel medium in order to maintain the topical application consistency. The average size, zeta potential, and polydispersity index for the 5-FU-NLC were found to be 208.32±8.21 nm, -21.82±0.40 mV, and 0.352±0.060, respectively. Transmission electron microscopy study revealed that 5-FU-NLC was <200 nm in size, with a spherical shape. In vitro drug permeation studies showed a release pattern with initial burst followed by sustained release, and the rate of 5-FU permeation was significantly improved for 5-FU-NLC gel (10.27±1.82 µg/cm2/h) as compared with plain 5-FU gel (2.85±1.12 µg/cm2/h). Further, skin retention studies showed a significant retention of 5-FU from the NLC gel (91.256±4.56 µg/cm2) as compared with that from the 5-FU plain gel (12.23±3.86 µg/cm2) in the rat skin. Skin irritation was also significantly reduced with 5-FU-NLC gel as compared with 5-FU plain gel. These results show that the prepared 5-FU-loaded NLC has high potential to improve the penetration of 5-FU through the stratum corneum, with enormous retention and with minimal skin irritation, which is the prerequisite for topically applied formulations. Keywords: nanostructured lipid carrier, topical delivery, controlled release, 5-fluorouracil, skin penetration, skin infection
format	article
author	Rajinikanth PS Chellian J
author_facet	Rajinikanth PS Chellian J
author_sort	Rajinikanth PS
title	Development and evaluation of nanostructured lipid carrier-based hydrogel for topical delivery of 5-fluorouracil
title_short	Development and evaluation of nanostructured lipid carrier-based hydrogel for topical delivery of 5-fluorouracil
title_full	Development and evaluation of nanostructured lipid carrier-based hydrogel for topical delivery of 5-fluorouracil
title_fullStr	Development and evaluation of nanostructured lipid carrier-based hydrogel for topical delivery of 5-fluorouracil
title_full_unstemmed	Development and evaluation of nanostructured lipid carrier-based hydrogel for topical delivery of 5-fluorouracil
title_sort	development and evaluation of nanostructured lipid carrier-based hydrogel for topical delivery of 5-fluorouracil
publisher	Dove Medical Press
publishDate	2016
url	https://doaj.org/article/723e6184da98422b8ef93c6cedba87ef
work_keys_str_mv	AT rajinikanthps developmentandevaluationofnanostructuredlipidcarrierbasedhydrogelfortopicaldeliveryof5fluorouracil AT chellianj developmentandevaluationofnanostructuredlipidcarrierbasedhydrogelfortopicaldeliveryof5fluorouracil
_version_	1718401495502684160

Development and evaluation of nanostructured lipid carrier-based hydrogel for topical delivery of 5-fluorouracil

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