Laffleur Flavia, Pschick Stefan, Barthelmes Jan, Hauptstein Sabine, Bernkop-Schnurch Andreas
Department of Pharmaceutical Technology, Institute of Pharmacy, Center for Molecular Biosciences Innsbruck, University of Innsbruck, Innrain 80/82, 6020 Innsbruck, Austria.
Curr Drug Deliv. 2018;15(3):351-356. doi: 10.2174/1567201814666170503142707.
It was the aim of this study to evaluate the impact of nonionic and ionic surfactants on skin penetration of dexpanthenol.
The relative potency of three surfactants (two nonionic and one ionic) as enhancers in the permeability of a series of compounds was investigated. The influence of the enhancers was also studied. For this purpose, porcine abdominal skin was prepared and mounted on Franz diffusion cells, while different mixtures of Dexpanthenol containing Tween®85, SDS and Span®80 in concentrations of 0.5%, 1%, 2%, 5% (m/V) were evaluated in terms of their permeation enhancing effect. The amount of permeated drug was determined via HPLC analysis. Moreover, the cytotoxicity and skin irritating effect of the compounds were tested on Caco-2 cells.
The cytotoxicity profile of Dexpanthenol showed no toxicity to the cells over 1 and 3 h of incubation. The permeation was evaluated over a time period of 180 min, whereas a ranking of SDS> Span>Tween could be determined as permeation enhancer.
Taking these findings into consideration, concentration of 1% (w/w) surfactant showed the most promising results. The increase in flux based on low concentrations of enhancer was ascribed to their ability to reduce skin´s barrier and improve drug permeation. The results showed that the nature of enhancer greatly impacts cutaneous barrier impairment.
本研究旨在评估非离子和离子表面活性剂对泛醇皮肤渗透的影响。
研究了三种表面活性剂（两种非离子型和一种离子型）作为一系列化合物渗透性增强剂的相对效能。还研究了增强剂的影响。为此，制备猪腹部皮肤并安装在Franz扩散池上，同时评估含有浓度为0.5%、1%、2%、5%（m/V）的吐温85、十二烷基硫酸钠（SDS）和司盘80的不同泛醇混合物的渗透增强效果。通过高效液相色谱分析测定渗透药物的量。此外，在Caco-2细胞上测试了这些化合物的细胞毒性和皮肤刺激作用。
泛醇的细胞毒性谱显示在孵育1小时和3小时后对细胞无毒性。在180分钟的时间段内评估渗透情况，确定SDS>司盘>吐温的渗透增强能力排序。
考虑到这些发现，1%（w/w）的表面活性剂浓度显示出最有前景的结果。基于低浓度增强剂的通量增加归因于它们降低皮肤屏障和改善药物渗透的能力。结果表明，增强剂的性质对皮肤屏障损伤有很大影响。
