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Molecules 2016, 21(2), 231; doi:10.3390/molecules21020231

Bioadhesive Surfactant Systems for Methotrexate Skin Delivery

1
Faculdade de Ciências Farmacêuticas, UNESP—Universidade Estadual Paulista, Campus Araraquara, Departamento de Fármacos e Medicamentos, Araraquara, SP, 14800-850, Brazil
2
Faculdade de Ciências Farmacêuticas, UNESP—Universidade Estadual Paulista, Campus Araraquara, Departamento de Análises Clínicas, Araraquara, SP 14800-850, Brazil
*
Authors to whom correspondence should be addressed.
Academic Editor: Alexandru Mihai Grumezescu
Received: 23 December 2015 / Revised: 2 February 2016 / Accepted: 5 February 2016 / Published: 18 February 2016
(This article belongs to the Special Issue Pharmaceutical Nanotechnology: Novel Approaches)
View Full-Text   |   Download PDF [1557 KB, uploaded 18 February 2016]   |  

Abstract

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. View Full-Text
Keywords: microemulsion; liquid-crystalline systems; in vitro skin permeation; in vitro skin retention; polyether functional siloxane; methotrexate microemulsion; liquid-crystalline systems; in vitro skin permeation; in vitro skin retention; polyether functional siloxane; methotrexate
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Cintra, G.A.S.; Pinto, L.A.; Calixto, G.M.F.; Soares, C.P.; Von Zuben, E.S.; Scarpa, M.V.; Gremião, M.P.D.; Chorilli, M. Bioadhesive Surfactant Systems for Methotrexate Skin Delivery. Molecules 2016, 21, 231.

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