表面活性剂对泛醇皮肤渗透的影响。

Impact of Surfactants on Skin Penetration of Dexpanthenol.

作者信息

Laffleur Flavia, Pschick Stefan, Barthelmes Jan, Hauptstein Sabine, Bernkop-Schnurch Andreas

机构信息

Department of Pharmaceutical Technology, Institute of Pharmacy, Center for Molecular Biosciences Innsbruck, University of Innsbruck, Innrain 80/82, 6020 Innsbruck, Austria.

出版信息

Curr Drug Deliv. 2018;15(3):351-356. doi: 10.2174/1567201814666170503142707.

DOI:10.2174/1567201814666170503142707

PMID:28472909

Abstract

OBJECTIVE

It was the aim of this study to evaluate the impact of nonionic and ionic surfactants on skin penetration of dexpanthenol.

METHODS

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.

RESULTS

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.

CONCLUSION

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.

摘要

目的

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。

方法

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。