Influence of different formulation variables on the performance of transdermal drug delivery system containing tizanidine hydrochloride: in vitro and ex vivo evaluations

Detalhes bibliográficos
Autor(a) principal: Shabbir, Maryam
Data de Publicação: 2018
Outros Autores: Ali, Sajid, Hamid, Irfan, Sharif, Ali, Akhtar, Muhammad Furqan, Raza, Moosa, Ahmed, Shoaib, Peerzada, Sohaib, Amin, Muhammad Umair
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Brazilian Journal of Pharmaceutical Sciences
Texto Completo: https://www.revistas.usp.br/bjps/article/view/159053
Resumo: The present study was aimed at preparation of transdermal patches of tizanidine HCl, evaluation of the effect of polymers on in vitro release pattern of the drug, and the effect of permeation enhancers on the penetration of the drug through the rabbit skin. Various proportions of hydrophilic (HPMC) and hydrophobic (Eudragit L-100) polymers were used with PEG 400 as film-forming agent, and Span 20 or DMSO as permeation enhancer. The formulations were assessed for physicochemical characteristics and in vitro drug release studies using USP paddle over disc method in phosphate buffered saline (pH 7.4) at 32.0±1°C. On the basis of in vitro studies and physicochemical evaluations, S03-A and S04-A were selected at Eudragit : HPMC ratios of 8 : 2 and 7 : 3, respectively, for further ex vivo analysis. The effects of different concentrations of Span 20 and DMSO were evaluated on excised rabbit skin using Franz diffusion cell. Cumulative drug permeation, flux, permeability coefficient, target flux, and enhancement ratio were calculated and compared with the control formulations. Kinetic models and Tukey’s multiple comparison test were applied to evaluate the drug release patterns. Formulation SB03- PE containing Eudragit L-100:HPMC (7:3) with Span 20 (15% w/w) produced the highest enhancement in drug permeation, and followed zero order kinetic model with super case-II drug release mechanism.
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spelling Influence of different formulation variables on the performance of transdermal drug delivery system containing tizanidine hydrochloride: in vitro and ex vivo evaluationsEx-vivo permeationEudragit L100Permeation enhancesTransdermal matrix patchMonolithic systemThe present study was aimed at preparation of transdermal patches of tizanidine HCl, evaluation of the effect of polymers on in vitro release pattern of the drug, and the effect of permeation enhancers on the penetration of the drug through the rabbit skin. Various proportions of hydrophilic (HPMC) and hydrophobic (Eudragit L-100) polymers were used with PEG 400 as film-forming agent, and Span 20 or DMSO as permeation enhancer. The formulations were assessed for physicochemical characteristics and in vitro drug release studies using USP paddle over disc method in phosphate buffered saline (pH 7.4) at 32.0±1°C. On the basis of in vitro studies and physicochemical evaluations, S03-A and S04-A were selected at Eudragit : HPMC ratios of 8 : 2 and 7 : 3, respectively, for further ex vivo analysis. The effects of different concentrations of Span 20 and DMSO were evaluated on excised rabbit skin using Franz diffusion cell. Cumulative drug permeation, flux, permeability coefficient, target flux, and enhancement ratio were calculated and compared with the control formulations. Kinetic models and Tukey’s multiple comparison test were applied to evaluate the drug release patterns. Formulation SB03- PE containing Eudragit L-100:HPMC (7:3) with Span 20 (15% w/w) produced the highest enhancement in drug permeation, and followed zero order kinetic model with super case-II drug release mechanism.Universidade de São Paulo. Faculdade de Ciências Farmacêuticas2018-12-20info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdfhttps://www.revistas.usp.br/bjps/article/view/15905310.1590/s2175-97902018000400130Brazilian Journal of Pharmaceutical Sciences; Vol. 54 Núm. 4 (2018); e00130Brazilian Journal of Pharmaceutical Sciences; v. 54 n. 4 (2018); e00130Brazilian Journal of Pharmaceutical Sciences; Vol. 54 No. 4 (2018); e001302175-97901984-8250reponame:Brazilian Journal of Pharmaceutical Sciencesinstname:Universidade de São Paulo (USP)instacron:USPenghttps://www.revistas.usp.br/bjps/article/view/159053/153983Copyright (c) 2018 Brazilian Journal of Pharmaceutical Sciencesinfo:eu-repo/semantics/openAccessShabbir, MaryamAli, SajidHamid, IrfanSharif, AliAkhtar, Muhammad FurqanRaza, MoosaAhmed, ShoaibPeerzada, SohaibAmin, Muhammad Umair2019-06-24T20:15:38Zoai:revistas.usp.br:article/159053Revistahttps://www.revistas.usp.br/bjps/indexPUBhttps://old.scielo.br/oai/scielo-oai.phpbjps@usp.br||elizabeth.igne@gmail.com2175-97901984-8250opendoar:2019-06-24T20:15:38Brazilian Journal of Pharmaceutical Sciences - Universidade de São Paulo (USP)false
dc.title.none.fl_str_mv Influence of different formulation variables on the performance of transdermal drug delivery system containing tizanidine hydrochloride: in vitro and ex vivo evaluations
title Influence of different formulation variables on the performance of transdermal drug delivery system containing tizanidine hydrochloride: in vitro and ex vivo evaluations
spellingShingle Influence of different formulation variables on the performance of transdermal drug delivery system containing tizanidine hydrochloride: in vitro and ex vivo evaluations
Shabbir, Maryam
Ex-vivo permeation
Eudragit L100
Permeation enhances
Transdermal matrix patch
Monolithic system
title_short Influence of different formulation variables on the performance of transdermal drug delivery system containing tizanidine hydrochloride: in vitro and ex vivo evaluations
title_full Influence of different formulation variables on the performance of transdermal drug delivery system containing tizanidine hydrochloride: in vitro and ex vivo evaluations
title_fullStr Influence of different formulation variables on the performance of transdermal drug delivery system containing tizanidine hydrochloride: in vitro and ex vivo evaluations
title_full_unstemmed Influence of different formulation variables on the performance of transdermal drug delivery system containing tizanidine hydrochloride: in vitro and ex vivo evaluations
title_sort Influence of different formulation variables on the performance of transdermal drug delivery system containing tizanidine hydrochloride: in vitro and ex vivo evaluations
author Shabbir, Maryam
author_facet Shabbir, Maryam
Ali, Sajid
Hamid, Irfan
Sharif, Ali
Akhtar, Muhammad Furqan
Raza, Moosa
Ahmed, Shoaib
Peerzada, Sohaib
Amin, Muhammad Umair
author_role author
author2 Ali, Sajid
Hamid, Irfan
Sharif, Ali
Akhtar, Muhammad Furqan
Raza, Moosa
Ahmed, Shoaib
Peerzada, Sohaib
Amin, Muhammad Umair
author2_role author
author
author
author
author
author
author
author
dc.contributor.author.fl_str_mv Shabbir, Maryam
Ali, Sajid
Hamid, Irfan
Sharif, Ali
Akhtar, Muhammad Furqan
Raza, Moosa
Ahmed, Shoaib
Peerzada, Sohaib
Amin, Muhammad Umair
dc.subject.por.fl_str_mv Ex-vivo permeation
Eudragit L100
Permeation enhances
Transdermal matrix patch
Monolithic system
topic Ex-vivo permeation
Eudragit L100
Permeation enhances
Transdermal matrix patch
Monolithic system
description The present study was aimed at preparation of transdermal patches of tizanidine HCl, evaluation of the effect of polymers on in vitro release pattern of the drug, and the effect of permeation enhancers on the penetration of the drug through the rabbit skin. Various proportions of hydrophilic (HPMC) and hydrophobic (Eudragit L-100) polymers were used with PEG 400 as film-forming agent, and Span 20 or DMSO as permeation enhancer. The formulations were assessed for physicochemical characteristics and in vitro drug release studies using USP paddle over disc method in phosphate buffered saline (pH 7.4) at 32.0±1°C. On the basis of in vitro studies and physicochemical evaluations, S03-A and S04-A were selected at Eudragit : HPMC ratios of 8 : 2 and 7 : 3, respectively, for further ex vivo analysis. The effects of different concentrations of Span 20 and DMSO were evaluated on excised rabbit skin using Franz diffusion cell. Cumulative drug permeation, flux, permeability coefficient, target flux, and enhancement ratio were calculated and compared with the control formulations. Kinetic models and Tukey’s multiple comparison test were applied to evaluate the drug release patterns. Formulation SB03- PE containing Eudragit L-100:HPMC (7:3) with Span 20 (15% w/w) produced the highest enhancement in drug permeation, and followed zero order kinetic model with super case-II drug release mechanism.
publishDate 2018
dc.date.none.fl_str_mv 2018-12-20
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv https://www.revistas.usp.br/bjps/article/view/159053
10.1590/s2175-97902018000400130
url https://www.revistas.usp.br/bjps/article/view/159053
identifier_str_mv 10.1590/s2175-97902018000400130
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv https://www.revistas.usp.br/bjps/article/view/159053/153983
dc.rights.driver.fl_str_mv Copyright (c) 2018 Brazilian Journal of Pharmaceutical Sciences
info:eu-repo/semantics/openAccess
rights_invalid_str_mv Copyright (c) 2018 Brazilian Journal of Pharmaceutical Sciences
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv Universidade de São Paulo. Faculdade de Ciências Farmacêuticas
publisher.none.fl_str_mv Universidade de São Paulo. Faculdade de Ciências Farmacêuticas
dc.source.none.fl_str_mv Brazilian Journal of Pharmaceutical Sciences; Vol. 54 Núm. 4 (2018); e00130
Brazilian Journal of Pharmaceutical Sciences; v. 54 n. 4 (2018); e00130
Brazilian Journal of Pharmaceutical Sciences; Vol. 54 No. 4 (2018); e00130
2175-9790
1984-8250
reponame:Brazilian Journal of Pharmaceutical Sciences
instname:Universidade de São Paulo (USP)
instacron:USP
instname_str Universidade de São Paulo (USP)
instacron_str USP
institution USP
reponame_str Brazilian Journal of Pharmaceutical Sciences
collection Brazilian Journal of Pharmaceutical Sciences
repository.name.fl_str_mv Brazilian Journal of Pharmaceutical Sciences - Universidade de São Paulo (USP)
repository.mail.fl_str_mv bjps@usp.br||elizabeth.igne@gmail.com
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