Physicochemical, in vitro and in vivo evaluation of flurbiprofen microemulsion

Detalhes bibliográficos
Autor(a) principal: NAEEM,MUHAMMAD
Data de Publicação: 2015
Outros Autores: RAHMAN,NISAR UR, TAVARES,GUILHERME. D., BARBOSA,SÁVIO F., CHACRA,NÁDIA B., LÖBENBERG,RAIMAR, SARFRAZ,MUHAMMAD K.
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Anais da Academia Brasileira de Ciências (Online)
Texto Completo: http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0001-37652015000401823
Resumo: ABSTRACTFlurbiprofen, a potent nonsteroidal anti-inflammatory drug, is widely used for relief of pain in patients suffering from rheumatic diseases, migraine, sore throat and primary dysmenorrheal. However, this drug has many gastrointestinal side effects produced by its oral administration, such as gastric bleeding and peptic ulcer. These effects were responsible for non-compliance among patients, which ultimately results in treatment failure. The physicochemical properties of flurbiprofen, make it a suitable candidate for transdermal drug delivery, which can overcome the drawbacks of oral administration. In this sense, microemulsions have been proved to increase the cutaneous absorption of lipophilic drugs when compared to conventional drug delivery systems. The purpose of this study was to formulate and characterize gel based microemulsions, for topical delivery of flurbiprofen. Different gel bases, containing microemulsion and hydro-alcoholic solution of flurbiprofen, were developed and compared. In vitro study showed that gels containing microemulsion had a higher permeation rate than those containing hydro-alcoholic solutions. Additionally, formulation of Carbopol-I (microemulsion) showed higher percent of inhibition of inflammation than others bases. Further, skin irritation study demonstrated that Carbopol-I was none irritating. Flurbiprofen microemulsion incorporated on Carbopol-I showed physicochemical, in vitro and in vivo characteristics suitable for the development of alternative transdermal delivery formulation.
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spelling Physicochemical, in vitro and in vivo evaluation of flurbiprofen microemulsionanti-inflammatory studyflurbiprofengelsIn vitro permeationmicroemulsionABSTRACTFlurbiprofen, a potent nonsteroidal anti-inflammatory drug, is widely used for relief of pain in patients suffering from rheumatic diseases, migraine, sore throat and primary dysmenorrheal. However, this drug has many gastrointestinal side effects produced by its oral administration, such as gastric bleeding and peptic ulcer. These effects were responsible for non-compliance among patients, which ultimately results in treatment failure. The physicochemical properties of flurbiprofen, make it a suitable candidate for transdermal drug delivery, which can overcome the drawbacks of oral administration. In this sense, microemulsions have been proved to increase the cutaneous absorption of lipophilic drugs when compared to conventional drug delivery systems. The purpose of this study was to formulate and characterize gel based microemulsions, for topical delivery of flurbiprofen. Different gel bases, containing microemulsion and hydro-alcoholic solution of flurbiprofen, were developed and compared. In vitro study showed that gels containing microemulsion had a higher permeation rate than those containing hydro-alcoholic solutions. Additionally, formulation of Carbopol-I (microemulsion) showed higher percent of inhibition of inflammation than others bases. Further, skin irritation study demonstrated that Carbopol-I was none irritating. Flurbiprofen microemulsion incorporated on Carbopol-I showed physicochemical, in vitro and in vivo characteristics suitable for the development of alternative transdermal delivery formulation.Academia Brasileira de Ciências2015-09-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersiontext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0001-37652015000401823Anais da Academia Brasileira de Ciências v.87 n.3 2015reponame:Anais da Academia Brasileira de Ciências (Online)instname:Academia Brasileira de Ciências (ABC)instacron:ABC10.1590/0001-3765201520130436info:eu-repo/semantics/openAccessNAEEM,MUHAMMADRAHMAN,NISAR URTAVARES,GUILHERME. D.BARBOSA,SÁVIO F.CHACRA,NÁDIA B.LÖBENBERG,RAIMARSARFRAZ,MUHAMMAD K.eng2015-09-22T00:00:00Zoai:scielo:S0001-37652015000401823Revistahttp://www.scielo.br/aabchttps://old.scielo.br/oai/scielo-oai.php||aabc@abc.org.br1678-26900001-3765opendoar:2015-09-22T00:00Anais da Academia Brasileira de Ciências (Online) - Academia Brasileira de Ciências (ABC)false
dc.title.none.fl_str_mv Physicochemical, in vitro and in vivo evaluation of flurbiprofen microemulsion
title Physicochemical, in vitro and in vivo evaluation of flurbiprofen microemulsion
spellingShingle Physicochemical, in vitro and in vivo evaluation of flurbiprofen microemulsion
NAEEM,MUHAMMAD
anti-inflammatory study
flurbiprofen
gels
In vitro permeation
microemulsion
title_short Physicochemical, in vitro and in vivo evaluation of flurbiprofen microemulsion
title_full Physicochemical, in vitro and in vivo evaluation of flurbiprofen microemulsion
title_fullStr Physicochemical, in vitro and in vivo evaluation of flurbiprofen microemulsion
title_full_unstemmed Physicochemical, in vitro and in vivo evaluation of flurbiprofen microemulsion
title_sort Physicochemical, in vitro and in vivo evaluation of flurbiprofen microemulsion
author NAEEM,MUHAMMAD
author_facet NAEEM,MUHAMMAD
RAHMAN,NISAR UR
TAVARES,GUILHERME. D.
BARBOSA,SÁVIO F.
CHACRA,NÁDIA B.
LÖBENBERG,RAIMAR
SARFRAZ,MUHAMMAD K.
author_role author
author2 RAHMAN,NISAR UR
TAVARES,GUILHERME. D.
BARBOSA,SÁVIO F.
CHACRA,NÁDIA B.
LÖBENBERG,RAIMAR
SARFRAZ,MUHAMMAD K.
author2_role author
author
author
author
author
author
dc.contributor.author.fl_str_mv NAEEM,MUHAMMAD
RAHMAN,NISAR UR
TAVARES,GUILHERME. D.
BARBOSA,SÁVIO F.
CHACRA,NÁDIA B.
LÖBENBERG,RAIMAR
SARFRAZ,MUHAMMAD K.
dc.subject.por.fl_str_mv anti-inflammatory study
flurbiprofen
gels
In vitro permeation
microemulsion
topic anti-inflammatory study
flurbiprofen
gels
In vitro permeation
microemulsion
description ABSTRACTFlurbiprofen, a potent nonsteroidal anti-inflammatory drug, is widely used for relief of pain in patients suffering from rheumatic diseases, migraine, sore throat and primary dysmenorrheal. However, this drug has many gastrointestinal side effects produced by its oral administration, such as gastric bleeding and peptic ulcer. These effects were responsible for non-compliance among patients, which ultimately results in treatment failure. The physicochemical properties of flurbiprofen, make it a suitable candidate for transdermal drug delivery, which can overcome the drawbacks of oral administration. In this sense, microemulsions have been proved to increase the cutaneous absorption of lipophilic drugs when compared to conventional drug delivery systems. The purpose of this study was to formulate and characterize gel based microemulsions, for topical delivery of flurbiprofen. Different gel bases, containing microemulsion and hydro-alcoholic solution of flurbiprofen, were developed and compared. In vitro study showed that gels containing microemulsion had a higher permeation rate than those containing hydro-alcoholic solutions. Additionally, formulation of Carbopol-I (microemulsion) showed higher percent of inhibition of inflammation than others bases. Further, skin irritation study demonstrated that Carbopol-I was none irritating. Flurbiprofen microemulsion incorporated on Carbopol-I showed physicochemical, in vitro and in vivo characteristics suitable for the development of alternative transdermal delivery formulation.
publishDate 2015
dc.date.none.fl_str_mv 2015-09-01
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
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dc.identifier.uri.fl_str_mv http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0001-37652015000401823
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dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv 10.1590/0001-3765201520130436
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
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dc.publisher.none.fl_str_mv Academia Brasileira de Ciências
publisher.none.fl_str_mv Academia Brasileira de Ciências
dc.source.none.fl_str_mv Anais da Academia Brasileira de Ciências v.87 n.3 2015
reponame:Anais da Academia Brasileira de Ciências (Online)
instname:Academia Brasileira de Ciências (ABC)
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instname_str Academia Brasileira de Ciências (ABC)
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reponame_str Anais da Academia Brasileira de Ciências (Online)
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repository.name.fl_str_mv Anais da Academia Brasileira de Ciências (Online) - Academia Brasileira de Ciências (ABC)
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