University Hospital and Clinic for Dermatology and Venereology, Martin Luther University Halle-Wittenberg, Halle (Saale), Germany.
Institute of Applied Dermatopharmacy, Martin Luther University Halle- Wittenberg, Halle (Saale), Germany.
J Dtsch Dermatol Ges. 2021 Apr;19(4):554-561. doi: 10.1111/ddg.14439. Epub 2021 Feb 15.
Keratolytics are often used to accelerate and improve the therapeutic response of hyperkeratotic dermatoses. Keratolytics are a chemically inhomogeneous group of substances and substance mixtures that clinically lead to a decrease in symptoms of a cornification disorder, but mediate different effects. Thus, keratolytic, keratoplastic, keratoemulsifying and keratodiluting effects are distinguished. The physicochemical effects or pharmacological efficacy of the respective keratolytics result in different mechanism as well as risks with regard to local or systemic compatibility. Until now, only little attention has been paid upon selection of keratolytics to the immediate consequences regarding diffusion conditions and pharmacokinetics of sequentially applied topicals, in particular of glucocorticoids.
This paper deals with the influence of keratolytics on the penetration-time profile of betamethasone dipropionate in sequential application. For this purpose, cutaneous bioavailability was investigated with the Franz chamber test using a tritium-labeled drug depending on the previous application of a keratolytic agent. Comparative data analyses were performed.
It was shown that keratoplastic substances significantly promote diffusion of the glucocorticoid. Keratoemulsifying substance mixtures exert no relevant effects in this regard, while keratodiluting substance mixtures inhibit penetration.
The targeted selection of a keratolytic can optimize the therapeutic effect and influence the bioavailability of sequentially applied topicals.
角质松解剂常用于加速和改善过度角化性皮肤病的治疗反应。角质松解剂是一组化学不均匀的物质和物质混合物，临床上可导致角化障碍症状的减轻，但介导不同的作用。因此，角质松解、角质塑型、角质乳化和角质稀释作用是有区别的。角质松解剂的理化作用或药理作用导致不同的机制以及局部或全身相容性的风险。到目前为止，对于顺序应用的局部用药物，特别是糖皮质激素，在选择角质松解剂时，仅很少关注其对扩散条件和药代动力学的直接影响。
本文研究了角质松解剂对角质松解后倍他米松二丙酸酯渗透时间曲线的影响。为此，使用放射性标记药物，通过Franz 室试验研究了角质松解剂顺序应用时的皮肤生物利用度。进行了比较数据分析。
结果表明，角质塑型物质显著促进了糖皮质激素的扩散。角质乳化物质混合物在这方面没有产生相关影响，而角质稀释物质混合物则抑制了渗透。
有针对性地选择角质松解剂可以优化治疗效果，并影响顺序应用的局部用药物的生物利用度。
