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Bioadhesive Surfactant Systems for Methotrexate Skin Delivery
Giovana Aparecida de Souza Cintra1, Larissa Alvarenga Pinto2, Giovana Maria Fioramonti Calixto3
1Faculdade de Ciências Farmacêuticas, UNESP-Universidade Estadual Paulista, Campus Araraquara, Departamento de Fármacos e Medicamentos, Araraquara, SP, 14800-850, Brazil. giovanacintra@gmail.com.
Molecules (Basel, Switzerland)
|February 23, 2016
Summary
New surfactant systems deliver methotrexate (MTX) effectively for skin diseases, reducing side effects. These bioadhesive microemulsions and liquid crystalline systems show potential for safer topical drug delivery.
Area of Science:
- Dermatology
- Materials Science
- Pharmaceutics
Background:
- Methotrexate (MTX) is an effective immunosuppressive drug for skin diseases.
- Systemic MTX use is limited by side effects like hepatotoxicity.
- Novel topical delivery systems are needed to improve MTX safety and efficacy.
Purpose of the Study:
- To develop and characterize novel surfactant systems for enhanced skin delivery of Methotrexate (MTX).
- To evaluate the physicochemical properties, in vitro release, and safety of MTX-loaded microemulsions (ME) and liquid crystalline systems (LCS).
Main Methods:
- Formulation of ME and LCS using silicone fluid, polyether functional siloxane (surfactant), and carbomer dispersion.
- Characterization using polarized light microscopy, small-angle X-ray scattering, texture analysis, and rheology.
- In vitro drug release studies and cytotoxicity assays on HaCaT cells.
Main Results:
- ME and LCS structures were confirmed, exhibiting hexagonal and lamellar phases.
- Formulations demonstrated suitable texture and bioadhesive properties for topical application.
- Controlled in vitro release of MTX was observed, best described by the Weibull model.
- MTX formulations were found to be non-cytotoxic to human keratinocytes.
Conclusions:
- Developed bioadhesive surfactant systems (ME and LCS) show promise for topical MTX delivery.
- These systems offer a potential strategy to mitigate MTX-related side effects.
- The study highlights the potential of polyether functional siloxane and carbomer-based systems for dermatological applications.
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