Bioadhesive Surfactant Systems for Methotrexate Skin Delivery

Detalhes bibliográficos
Autor(a) principal: Cintra, Giovana Aparecida de Souza
Data de Publicação: 2016
Outros Autores: Pinto, Larissa Alvarenga, Calixto, Giovana Maria Fioramonti, Soares, Christiane Pienna, Von Zuben, Eliete de Souza, Scarpa, Maria Virgínia, Gremião, Maria Palmira Daflon, Chorilli, Marlus
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Repositório Institucional da UNESP
Texto Completo: http://dx.doi.org/10.3390/molecules21020231
http://hdl.handle.net/11449/177140
Resumo: Methotrexate (MTX) is an immunosuppressive drug for systemic use in the treatment of skin diseases, however, MTX presents a number of side effects, such as hepatotoxicity. To overcome this limitation, this study developed skin MTX delivery surfactant systems, such as a microemulsion (ME) and a liquid crystalline system (LCS), consisting of a glycol copolymer-based silicone fluid (SFGC) as oil phase, polyether functional siloxane (PFS) as surfactant, and carbomer homopolymer type A (C971) dispersion at 0.5% (wt/wt) as aqueous phase. Polarized light microscopy and small-angle X-ray scattering evidenced the presence of hexagonal and lamellar LCSs, and also a ME. Texture profile and in vitro bioadhesion assays showed that these formulations are suitable for topical application, showing interesting hardness, adhesiveness and compressibility values. Rheology analysis confirmed the Newtonian behaviour of the ME, whereas lamellar and hexagonal LCSs behave as pseudoplastic and dilatant non-Newtonian fluids, respectively. In vitro release profiles indicated that MTX could be released in a controlled manner from all the systems, and the Weibull model showed the highest adjusted coefficient of determination. Finally, the formulations were not cytotoxic to the immortalized human keratinocyte line HaCaT. Therefore, these bioadhesive surfactant systems established with PFS and C971 have great potential as skin delivery systems.
id UNSP_fc645e86a93157cd5d8e9cf036f88838
oai_identifier_str oai:repositorio.unesp.br:11449/177140
network_acronym_str UNSP
network_name_str Repositório Institucional da UNESP
repository_id_str 2946
spelling Bioadhesive Surfactant Systems for Methotrexate Skin Deliveryin vitro skin permeationin vitro skin retentionliquid-crystalline systemsmethotrexatemicroemulsionpolyether functional siloxaneMethotrexate (MTX) is an immunosuppressive drug for systemic use in the treatment of skin diseases, however, MTX presents a number of side effects, such as hepatotoxicity. To overcome this limitation, this study developed skin MTX delivery surfactant systems, such as a microemulsion (ME) and a liquid crystalline system (LCS), consisting of a glycol copolymer-based silicone fluid (SFGC) as oil phase, polyether functional siloxane (PFS) as surfactant, and carbomer homopolymer type A (C971) dispersion at 0.5% (wt/wt) as aqueous phase. Polarized light microscopy and small-angle X-ray scattering evidenced the presence of hexagonal and lamellar LCSs, and also a ME. Texture profile and in vitro bioadhesion assays showed that these formulations are suitable for topical application, showing interesting hardness, adhesiveness and compressibility values. Rheology analysis confirmed the Newtonian behaviour of the ME, whereas lamellar and hexagonal LCSs behave as pseudoplastic and dilatant non-Newtonian fluids, respectively. In vitro release profiles indicated that MTX could be released in a controlled manner from all the systems, and the Weibull model showed the highest adjusted coefficient of determination. Finally, the formulations were not cytotoxic to the immortalized human keratinocyte line HaCaT. Therefore, these bioadhesive surfactant systems established with PFS and C971 have great potential as skin delivery systems.Faculdade de Ciências Farmacêuticas, UNESP-Universidade Estadual Paulista, Campus Araraquara, Departamento de Fármacos e Medicamentos, Araraquara, SP, 14800-850, BrazilFaculdade de Ciências Farmacêuticas, UNESP-Universidade Estadual Paulista, Campus Araraquara, Departamento de Fármacos e Medicamentos, Araraquara, SP, 14800-850, Brazil. larissa_alvarenga@ymail.comFaculdade de Ciências Farmacêuticas, UNESP-Universidade Estadual Paulista, Campus Araraquara, Departamento de Análises Clínicas, Araraquara, SP 14800-850, BrazilFaculdade de Ciências Farmacêuticas, UNESP-Universidade Estadual Paulista, Campus Araraquara, Departamento de Fármacos e Medicamentos, Araraquara, SP, 14800-850, Brazil. eliete.vz@gmail.comFaculdade de Ciências Farmacêuticas, UNESP-Universidade Estadual Paulista, Campus Araraquara, Departamento de Fármacos e Medicamentos, Araraquara, SP, 14800-850, Brazil. pgremiao@fcfar.unesp.brUniversidade Estadual Paulista (Unesp)Cintra, Giovana Aparecida de SouzaPinto, Larissa AlvarengaCalixto, Giovana Maria FioramontiSoares, Christiane PiennaVon Zuben, Eliete de SouzaScarpa, Maria VirgíniaGremião, Maria Palmira DaflonChorilli, Marlus2018-12-11T17:24:11Z2018-12-11T17:24:11Z2016-02-18info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articleapplication/pdfhttp://dx.doi.org/10.3390/molecules21020231Molecules (Basel, Switzerland), v. 21, n. 2, 2016.1420-3049http://hdl.handle.net/11449/17714010.3390/molecules210202312-s2.0-850475852782-s2.0-85047585278.pdf91297805367242564930795298045665142712599671628217680252903736690000-0003-1740-7360Scopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengMolecules (Basel, Switzerland)0,855info:eu-repo/semantics/openAccess2024-06-24T13:46:13Zoai:repositorio.unesp.br:11449/177140Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-08-05T21:39:02.841790Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false
dc.title.none.fl_str_mv Bioadhesive Surfactant Systems for Methotrexate Skin Delivery
title Bioadhesive Surfactant Systems for Methotrexate Skin Delivery
spellingShingle Bioadhesive Surfactant Systems for Methotrexate Skin Delivery
Cintra, Giovana Aparecida de Souza
in vitro skin permeation
in vitro skin retention
liquid-crystalline systems
methotrexate
microemulsion
polyether functional siloxane
title_short Bioadhesive Surfactant Systems for Methotrexate Skin Delivery
title_full Bioadhesive Surfactant Systems for Methotrexate Skin Delivery
title_fullStr Bioadhesive Surfactant Systems for Methotrexate Skin Delivery
title_full_unstemmed Bioadhesive Surfactant Systems for Methotrexate Skin Delivery
title_sort Bioadhesive Surfactant Systems for Methotrexate Skin Delivery
author Cintra, Giovana Aparecida de Souza
author_facet Cintra, Giovana Aparecida de Souza
Pinto, Larissa Alvarenga
Calixto, Giovana Maria Fioramonti
Soares, Christiane Pienna
Von Zuben, Eliete de Souza
Scarpa, Maria Virgínia
Gremião, Maria Palmira Daflon
Chorilli, Marlus
author_role author
author2 Pinto, Larissa Alvarenga
Calixto, Giovana Maria Fioramonti
Soares, Christiane Pienna
Von Zuben, Eliete de Souza
Scarpa, Maria Virgínia
Gremião, Maria Palmira Daflon
Chorilli, Marlus
author2_role author
author
author
author
author
author
author
dc.contributor.none.fl_str_mv Universidade Estadual Paulista (Unesp)
dc.contributor.author.fl_str_mv Cintra, Giovana Aparecida de Souza
Pinto, Larissa Alvarenga
Calixto, Giovana Maria Fioramonti
Soares, Christiane Pienna
Von Zuben, Eliete de Souza
Scarpa, Maria Virgínia
Gremião, Maria Palmira Daflon
Chorilli, Marlus
dc.subject.por.fl_str_mv in vitro skin permeation
in vitro skin retention
liquid-crystalline systems
methotrexate
microemulsion
polyether functional siloxane
topic in vitro skin permeation
in vitro skin retention
liquid-crystalline systems
methotrexate
microemulsion
polyether functional siloxane
description Methotrexate (MTX) is an immunosuppressive drug for systemic use in the treatment of skin diseases, however, MTX presents a number of side effects, such as hepatotoxicity. To overcome this limitation, this study developed skin MTX delivery surfactant systems, such as a microemulsion (ME) and a liquid crystalline system (LCS), consisting of a glycol copolymer-based silicone fluid (SFGC) as oil phase, polyether functional siloxane (PFS) as surfactant, and carbomer homopolymer type A (C971) dispersion at 0.5% (wt/wt) as aqueous phase. Polarized light microscopy and small-angle X-ray scattering evidenced the presence of hexagonal and lamellar LCSs, and also a ME. Texture profile and in vitro bioadhesion assays showed that these formulations are suitable for topical application, showing interesting hardness, adhesiveness and compressibility values. Rheology analysis confirmed the Newtonian behaviour of the ME, whereas lamellar and hexagonal LCSs behave as pseudoplastic and dilatant non-Newtonian fluids, respectively. In vitro release profiles indicated that MTX could be released in a controlled manner from all the systems, and the Weibull model showed the highest adjusted coefficient of determination. Finally, the formulations were not cytotoxic to the immortalized human keratinocyte line HaCaT. Therefore, these bioadhesive surfactant systems established with PFS and C971 have great potential as skin delivery systems.
publishDate 2016
dc.date.none.fl_str_mv 2016-02-18
2018-12-11T17:24:11Z
2018-12-11T17:24:11Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://dx.doi.org/10.3390/molecules21020231
Molecules (Basel, Switzerland), v. 21, n. 2, 2016.
1420-3049
http://hdl.handle.net/11449/177140
10.3390/molecules21020231
2-s2.0-85047585278
2-s2.0-85047585278.pdf
9129780536724256
4930795298045665
1427125996716282
1768025290373669
0000-0003-1740-7360
url http://dx.doi.org/10.3390/molecules21020231
http://hdl.handle.net/11449/177140
identifier_str_mv Molecules (Basel, Switzerland), v. 21, n. 2, 2016.
1420-3049
10.3390/molecules21020231
2-s2.0-85047585278
2-s2.0-85047585278.pdf
9129780536724256
4930795298045665
1427125996716282
1768025290373669
0000-0003-1740-7360
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv Molecules (Basel, Switzerland)
0,855
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.source.none.fl_str_mv Scopus
reponame:Repositório Institucional da UNESP
instname:Universidade Estadual Paulista (UNESP)
instacron:UNESP
instname_str Universidade Estadual Paulista (UNESP)
instacron_str UNESP
institution UNESP
reponame_str Repositório Institucional da UNESP
collection Repositório Institucional da UNESP
repository.name.fl_str_mv Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)
repository.mail.fl_str_mv
_version_ 1808129343943081984