ABSTRACT

Acitretin is the drug of choice for the treatment of psoriasis, but due to its poor solubility, the development of oral and topical formulations of acitretin has been restricted. The aim of the present investigation was to enhance the solubility of acitretin. Solid dispersions of acitretin were prepared using a lipidic solubilizer, Gelucire® 44/14. These solid dispersions were characterized through FT-IR, DSC, XRD, drug content and solubility studies. The most solubilized dispersion was loaded on an N,N-methylenebisacrylamide microporous cryogel. Physical parameters of the solubilized drug such as the porosity, rheological behaviour, surface properties, appearance, drug content and diffusion behaviour were studied. It was concluded that the solubilized form of acitretin, loaded on a surface-modified cryogel, is the best option for the treatment of psoriasis. The hydration of the skin was excellent, and the permeability of the acitretin into the skin was better.

摘要

阿维A是治疗银屑病的首选药物，但由于其溶解性差，阿维A口服和外用制剂的开发受到限制。本研究的目的是提高阿曲汀的溶解度。使用脂质增溶剂 Gelucire® 44/14 制备阿曲汀的固体分散体。通过 FT-IR、DSC、XRD、药物含量和溶解度研究对这些固体分散体进行了表征。最溶解的分散体装载在 N,N-亚甲基双丙烯酰胺微孔冷冻凝胶上。研究了溶解药物的物理参数，例如孔隙率、流变行为、表面性质、外观、药物含量和扩散行为。得出的结论是，负载在表面改性冷冻凝胶上的溶解形式的阿曲汀，是治疗牛皮癣的最佳选择。皮肤的水合作用非常好，阿维A对皮肤的渗透性更好。