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经皮给药系统成为近年来药物制剂开发研究的热点,皮肤角质层脂质的屏障功能是限制其开发应用的最大因素。本文采用计算机模拟技术成功搭建了角质层脂质模型,并对其稳定性进行了考察。结果表明,组成比为神经酰胺:胆固醇:游离脂肪酸=2:2:1的模型不仅能够合理地解释皮肤角质层的屏障特性,并具备应对水合程度、离子强度和pH变化的很好的稳定性。研究结果为深入阐明经皮给药系统与胞间脂质层的相互作用奠定了基础,对于经皮给药系统的研发具有一定的意义。
Transdermal drug delivery system has become a hot spot in the research and development of drug formulations in recent years. The barrier function of cuticular lipid in the skin is the biggest factor limiting its development and application. In this paper, the stratum corneum lipids model was successfully established by computer simulation and its stability was investigated. The results showed that the model with a compositional ratio of ceramide: cholesterol: free fatty acid = 2: 2: 1 not only can reasonably explain the barrier properties of the stratum corneum, but also has good stability against changes in hydration, ionic strength and pH . The results lay a foundation for further clarifying the interaction between the transdermal delivery system and the intercellular lipid layer and have certain significance for the development of transdermal drug delivery system.