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.
Highlights
Methotrexate (MTX), known as amethopterin whose structure is shown in Figure 1, is a cytotoxic antifolate drug approved by U.S Food and Drug Administration (FDA) as an anti-psoriatic agent since 1971 [1]
This study demonstrated that the proposed systems containing polyether functional siloxane as a surfactant, silicone glycol copolymer fluid as oil phase, and an aqueous phase comprising an aqueous dispersion containing 0.5% of C971 are effective in the controlled release of MTX, presenting texture profile and bioadhesion suitable for skin use
The results showed that the structural modifications of the system could modify the rate and profile of drug delivery
Summary
Methotrexate (MTX), known as amethopterin whose structure is shown in Figure 1, is a cytotoxic antifolate drug approved by U.S Food and Drug Administration (FDA) as an anti-psoriatic agent since 1971 [1]. Methotrexate (MTX), known as amethopterin whose structure is shown, is a cytotoxic antifolate drug approved by U.S Food and Drug Administration (FDA) as an anti-psoriatic agent since 1971 [1]. It is one of the most prominent substances used systemically in the treatment of psoriasis and it is used in cancer treatment as a cytostatic agent. Medical treatment for skin conditions complements the medical in patients. Medical treatment for skin conditions complements the medical therapy therapy of psychological psychological health
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