Prasad Rachna, Koul Veena
Centre for Biomedical Engineering, Indian Institute of Technology, Hauz Khas, New Delhi 110016, India.
Ther Deliv. 2012 Mar;3(3):315-25. doi: 10.4155/tde.12.3.
Mehotrexate has been reported as an immunosuppressant and an antimetabolite widely used in the treatment of rheumatoid arthritis and psoriasis. However, it causes various toxicities and has low bioavailability when taken orally, thus, it is desirable that the drug be delivered transdermally. The water solubility and charged structure of methotrexate, however, limits its use via the transdermal route mainly due to the highly organized microstructure of the stratum corneum. Hence, various technologies, such as chemical enhancers, iontophoresis, electroporation, ultrasound and microneedles, either alone or in combination, are being explored to enhance its permeability by disrupting the barrier property of the skin. The present article discusses the past, present and future of transdermal delivery of methotrexate.
据报道，甲氨蝶呤作为一种免疫抑制剂和抗代谢物，广泛应用于类风湿性关节炎和银屑病的治疗。然而，它会引起各种毒性，口服时生物利用度低，因此，希望通过透皮给药。然而，甲氨蝶呤的水溶性和带电结构限制了其经皮途径的使用，这主要是由于角质层高度有序的微观结构。因此，人们正在探索各种技术，如化学增强剂、离子导入、电穿孔、超声和微针，单独或联合使用，以通过破坏皮肤的屏障特性来提高其渗透性。本文讨论了甲氨蝶呤透皮给药的过去、现在和未来。
