Bioadhesive Surfactant Systems for Methotrexate Skin Delivery
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 liqui...
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| Format: | Article |
| Language: | English |
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MDPI AG
2016-02-01
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| Series: | Molecules |
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| Online Access: | http://www.mdpi.com/1420-3049/21/2/231 |
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| author | Giovana Aparecida de Souza Cintra Larissa Alvarenga Pinto Giovana Maria Fioramonti Calixto Christiane Pienna Soares Eliete de Souza Von Zuben Maria Virgínia Scarpa Maria Palmira Daflon Gremião Marlus Chorilli |
| author_facet | Giovana Aparecida de Souza Cintra Larissa Alvarenga Pinto Giovana Maria Fioramonti Calixto Christiane Pienna Soares Eliete de Souza Von Zuben Maria Virgínia Scarpa Maria Palmira Daflon Gremião Marlus Chorilli |
| author_sort | Giovana Aparecida de Souza Cintra |
| collection | DOAJ |
| 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. |
| first_indexed | 2024-12-21T14:44:27Z |
| format | Article |
| id | doaj.art-b2b0569f2ad8484fa80183deeb97f1d3 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-21T14:44:27Z |
| publishDate | 2016-02-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-b2b0569f2ad8484fa80183deeb97f1d32022-12-21T19:00:04ZengMDPI AGMolecules1420-30492016-02-0121223110.3390/molecules21020231molecules21020231Bioadhesive Surfactant Systems for Methotrexate Skin DeliveryGiovana Aparecida de Souza Cintra0Larissa Alvarenga Pinto1Giovana Maria Fioramonti Calixto2Christiane Pienna Soares3Eliete de Souza Von Zuben4Maria Virgínia Scarpa5Maria Palmira Daflon Gremião6Marlus Chorilli7Faculdade 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, BrazilFaculdade 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 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, BrazilFaculdade 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, BrazilFaculdade de Ciências Farmacêuticas, UNESP—Universidade Estadual Paulista, Campus Araraquara, Departamento de Fármacos e Medicamentos, Araraquara, SP, 14800-850, BrazilMethotrexate (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.http://www.mdpi.com/1420-3049/21/2/231microemulsionliquid-crystalline systemsin vitro skin permeationin vitro skin retentionpolyether functional siloxanemethotrexate |
| spellingShingle | Giovana Aparecida de Souza Cintra Larissa Alvarenga Pinto Giovana Maria Fioramonti Calixto Christiane Pienna Soares Eliete de Souza Von Zuben Maria Virgínia Scarpa Maria Palmira Daflon Gremião Marlus Chorilli Bioadhesive Surfactant Systems for Methotrexate Skin Delivery Molecules microemulsion liquid-crystalline systems in vitro skin permeation in vitro skin retention polyether functional siloxane methotrexate |
| title | 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_short | Bioadhesive Surfactant Systems for Methotrexate Skin Delivery |
| title_sort | bioadhesive surfactant systems for methotrexate skin delivery |
| topic | microemulsion liquid-crystalline systems in vitro skin permeation in vitro skin retention polyether functional siloxane methotrexate |
| url | http://www.mdpi.com/1420-3049/21/2/231 |
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