School of Applied Sciences, University of Huddersfield, Queensgate, Huddersfield HD1 3DH, UK.
School of Applied Sciences, University of Huddersfield, Queensgate, Huddersfield HD1 3DH, UK.
J Pharm Sci. 2020 Jun;109(6):2033-2037. doi: 10.1016/j.xphs.2020.03.007. Epub 2020 Mar 13.
This work evaluates permeation of 12 model pharmaceutical compounds through a chemically modified form of poly(dimethylsiloxane), whereby the polymer surface had undergone silanization. Standard polymer membrane has been widely used as a simplified skin model to investigate transdermal permeation yet does not fully mimic human skin. The surface chemistry of modified polymer was investigated such as the ability to bind to drugs, hydrophobicity and pore size using optical microscopy, the Brunauer-Emmett-Teller technique and Fourier-transform infrared spectroscopy, followed by permeation analysis with UV spectroscopy. For 11 of the 12 compounds, an appreciable increase in the extent of permeation was observed after 6 h when using the silanized polymer compared with the standard poly(dimethylsiloxane). Furthermore, a correlation was found between the degree of permeation increase and hydrophobicity (logP) of the drug (R = 0.90). These findings indicate that permeation can be controlled by modifying the membrane surface, although the hydrophobicity of the permeant also plays a vital role in the extent of permeation observed. This concept study presents a potential alternative membrane for pharmaceutical transdermal analysis, providing many benefits over existing options.
本工作评估了 12 种模型药物化合物通过化学改性聚二甲基硅氧烷(PDMS)的渗透情况,其中聚合物表面经历了硅烷化处理。标准聚合物膜已被广泛用作简化的皮肤模型来研究经皮渗透,但不能完全模拟人体皮肤。使用光学显微镜、BET 技术和傅里叶变换红外光谱法研究了改性聚合物的表面化学性质,如与药物结合的能力、疏水性和孔径,然后通过紫外光谱法进行渗透分析。对于 12 种化合物中的 11 种,与标准 PDMS 相比,使用硅烷化聚合物后,在 6 小时后观察到渗透程度明显增加。此外,还发现渗透增加的程度与药物的疏水性(logP)之间存在相关性(R=0.90)。这些发现表明,可以通过修饰膜表面来控制渗透,尽管渗透物的疏水性在观察到的渗透程度中也起着至关重要的作用。本概念研究为药物经皮分析提供了一种潜在的替代膜,与现有选择相比具有许多优势。