Department of Pharmaceutical Technology, Faculty of Science, Eberhard Karls Universität Tübingen, Auf der Morgenstelle 8, 72076 Tuebingen, Germany.
Department of Pharmaceutical Technology, Faculty of Science, Eberhard Karls Universität Tübingen, Auf der Morgenstelle 8, 72076 Tuebingen, Germany.
Eur J Pharm Biopharm. 2021 Sep;166:1-9. doi: 10.1016/j.ejpb.2021.04.027. Epub 2021 Jun 1.
Non-ionic emulsifiers have been continuous research focus in skin analysis. With the aim of finding their role as penetration enhancers in dermal drug delivery systems, PEGylated emulsifiers of polyethylene glycol (PEG) ethers were targeted to be investigated ex-vivo. The effectiveness of them in the enhancement of skin penetration was examined by conventional tape stripping method and confocal Raman spectroscopy (CRS). Fluorescein sodium salt (Fluo-Na) and procaine HCl were respectively used as model drugs. The drug delivery performances were compared in the aspects of penetration amount and depth. Based on the results from both analyses, all investigated emulsifiers have the ability to enhance the amount of drug penetration. PEG-20 ethers showed higher ability than PEG-2 oleyl ether (O2) in promoting drug distribution by depth, especially PEG-20 cetyl ether (C20) showed a distinct effect. According to this study, their penetration enhancing performances seem to be linked to their interruption of intercellular lipids, which can be considered as the underlying mechanism for governing the ability of PEGylated emulsifiers as penetration enhancers. Further instrumental comparison highlighted the benefits of using CRS as an alternative in skin penetration analysis.
非离子型乳化剂一直是皮肤分析的研究重点。本研究旨在寻找其作为经皮给药系统中渗透增强剂的作用，以聚乙二醇（PEG）醚的聚乙二醇化乳化剂为目标进行体外研究。通过常规胶带剥离法和共聚焦拉曼光谱（CRS）研究了它们对皮肤渗透增强的效果。分别使用荧光素钠（Fluo-Na）和盐酸普鲁卡因作为模型药物。从渗透量和深度两方面比较了药物的传递性能。基于这两种分析的结果，所有研究的乳化剂都具有增强药物渗透量的能力。PEG-20 醚比 PEG-2 油基醚（O2）更有能力通过深度促进药物分布，特别是 PEG-20 鲸蜡基醚（C20）表现出明显的效果。根据这项研究，它们的渗透增强性能似乎与其对细胞间脂质的干扰有关，这可以被认为是控制聚乙二醇化乳化剂作为渗透增强剂能力的潜在机制。进一步的仪器比较强调了使用 CRS 作为皮肤渗透分析替代方法的好处。
