Asbill CS, Michniak BB
Dept of Basic Pharmaceutical Sciences, College of Pharmacy, University of South Carolina, Columbia, SC 29208, USA.
Pharm Sci Technol Today. 2000 Jan;3(1):36-41. doi: 10.1016/s1461-5347(99)00225-4.
The stratum corneum, poses a formidable challenge to formulators of drug delivery systems. Several approaches have been utilized to facilitate entry of drugs into the lower skin layers. Traditionally, permeation enhancers were designed to deliver high drug concentrations across the skin into the systemic circulation. The use of many of these agents resulted in unpleasant or toxic side effects. However, in recent years there has been a search for compounds that exhibit low toxicity, and maintain their enhancing activity. More recently, there has been interest in agents that may be used in topical formulations to prevent the passage of active ingredients or excipients into the lower skin layers. These so-called skin retardants have potential uses in many over-the-counter (OTC) skin formulations, such as sunscreens and pesticides, where the site of action is restricted to the skin surface or upper skin layers. Research in the area of permeation enhancement or retardation is yielding valuable insights into the structure-activity relationships of enhancers as well as retardants.
角质层对药物递送系统的配方设计师构成了巨大挑战。人们已经采用了几种方法来促进药物进入皮肤下层。传统上，渗透促进剂旨在将高浓度药物透过皮肤输送到体循环中。使用其中许多药剂会产生不良或毒性副作用。然而，近年来一直在寻找毒性低且能保持其增强活性的化合物。最近，人们对可用于局部制剂以防止活性成分或辅料进入皮肤下层的药剂产生了兴趣。这些所谓的皮肤阻滞剂在许多非处方（OTC）皮肤制剂中具有潜在用途，如防晒霜和杀虫剂，其作用部位仅限于皮肤表面或皮肤上层。渗透增强或阻滞领域的研究正在为促进剂和阻滞剂的构效关系提供有价值的见解。
