Arellano A, Santoyo S, Martn C, Ygartua P
Departamento de Farmacia y Tecnologia Farmacéutica, Facultad de Farmacia, Universidad de Navarra, Pamplona, Spain.
Eur J Drug Metab Pharmacokinet. 1998 Apr-Jun;23(2):307-12. doi: 10.1007/BF03189356.
Nonionic surfactants, which are a safe class of enhancers, may offer means of enhancing drug permeation through the skin. In order to determine this effect, the influence of four nonionic surfactants on the percutaneous absorption of diclofenac sodium from carbopol gels containing 40% propylene glycol was investigated. In vitro diffusion experiments were carried out using excised full-thickness abdominal rat skin as well as cellulose nitrate membranes. The data of this study clearly revealed that Tween 80 decreased diclofenac penetration rate. This was due to a decrease in thermodynamic activity as a result of micellar complexation. In contrast, the more hydrophobic sorbitans enhanced diclofenac skin penetration, probably due to changes in the barrier properties of the skin and in the vehicle-stratum corneum partition coefficient. The most enhancing effect was induced by Span 20, a surfactant with a C12 saturated hydrophobic group. However, diffusional lag times for all the tested surfactants were longer than for the control gel.
非离子表面活性剂是一类安全的促进剂，可能提供增强药物经皮渗透的方法。为了确定这种效果，研究了四种非离子表面活性剂对含40%丙二醇的卡波姆凝胶中双氯芬酸钠经皮吸收的影响。使用切除的大鼠全层腹部皮肤以及硝酸纤维素膜进行体外扩散实验。本研究数据清楚地表明，吐温80降低了双氯芬酸的渗透速率。这是由于胶束络合导致热力学活性降低。相比之下，疏水性更强的脱水山梨醇酯增强了双氯芬酸的皮肤渗透，这可能是由于皮肤屏障特性和载体-角质层分配系数的变化。增强效果最显著的是司盘20，一种具有C12饱和疏水基团的表面活性剂。然而，所有测试表面活性剂的扩散滞后时间都比对照凝胶长。
