The potential of metabolic interventions to enhance transdermal drug delivery
The potential of metabolic interventions to enhance transdermal drug delivery
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DOI：
10.1046/j.1523-1747.2002.19632.x
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发表时间：
2002-12-01
影响因子：
--
通讯作者：
Feingold, KR
中科院分区：
文献类型：
--
作者：
Elias, PM;Tsai, J;Feingold, KR
角质层是一种复杂的组织，具有代谢活性，并且由于存在几种自调节酶系统而经历动态结构修饰。大量的防御（保护）功能体现在这个组织中，每一个都有自己的结构和生化基础。此外，角质层对渗透性屏障的外部扰动有反应，上调旨在恢复正常屏障功能的各种代谢过程。传统的药物递送方法，其有效性有限，将角质层视为静止的但半渗透的膜。相比之下，新的基于代谢的方法，可以单独使用，或与标准方法结合使用，已被证明可以扩大药物的范围，可以在无毛小鼠表皮透皮递送。然而，虽然这些新方法有很大的希望，如果在人类皮肤中同样有效，它们提出了关于高度渗透角质层风险的新问题。
The stratum corneum is a complex tissue that is metabolically active, and undergoes dynamic structural modifications due to the presence of several self-regulating enzymatic systems. A large number of defensive (protective) functions are embodied in this tissue, each with its own structural and biochemical basis. Moreover, the stratum corneum is responsive to external perturbations to the permeability barrier, upregulating a variety of metabolic processes aimed at restoring normal barrier function. Traditional drug delivery methods, which are of limited effectiveness, view the stratum corneum as a static, but semipermeable membrane. In contrast, newer metabolically based methods, which can be deployed alone, or in conjunction with standard methods, have been shown to expand the spectrum of drugs that can be delivered transdermally in hairless mouse epidermis. Yet, while these new approaches hold great promise, if equally effective in human skin, they pose new questions about the risks of a highly permeabilized stratum corneum.