Non-ionic surfactants as innovative skin penetration enhancers: insight in the mechanism of interaction with simple 2D stratum corneum model system

角质层 化学 渗透(战争) 肺表面活性物质 透皮 单层 色谱法 溶解度 衰减全反射 化学工程 生物物理学 有机化学 生物化学 红外光谱学 药理学 工程类 病理 生物 医学 运筹学
作者
Fabio Strati,Reinhard H.H. Neubert,Lukáš Opálka,Andreas Kerth,Gerald Brezesinski
出处
期刊:European Journal of Pharmaceutical Sciences [Elsevier BV]
卷期号:157: 105620-105620 被引量:21
标识
DOI:10.1016/j.ejps.2020.105620
摘要

Transdermal drug delivery is a passive diffusion process of an active compound through the skin which is affected by drug solubility in the multilamellar lipidic matrix of the stratum corneum (SC). Widely used non-ionic surfactants (NIS) can be added into transdermal formulations to enhance the penetration of drugs by influencing the packing of the stratum corneum lipidic matrix. Objective of our study was to analyse the interaction between selected NIS and a simple SC lipidic matrix model system using a variety of surface-sensitive techniques based on the application of Langmuir monolayers. In this work, the well-known surfactant Polysorbate 80 was compared with a modern surfactant Sucrose monolaurate. Infrared reflection-absorption spectroscopy (IRRAS) and epifluorescence microscopy provide information about the effects of those surfactants on the SC model system. Monolayer isotherms of the SC model mixture indicate a very stiff and well-packed layer, however, packing defects are evidenced in epifluorescence studies. The injection of the two NIS underneath the SC monolayers proved their potential to penetrate into the SC model at the air-water interface having a maximum insertion pressure (MIP) above the assumed lateral pressure of biological membranes. The NIS adsorbed preferentially into packing defects seen in epifluorescence microscopy studies with Sucrose monolaurate being more active than Polysorbate 80 in disordering the SC monolayer.
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