Profiling skin penetration using PEGylated emulsifiers as penetration enhancers via confocal Raman spectroscopy and fluorescence spectroscopy
Profiling skin penetration using PEGylated emulsifiers as penetration enhancers via confocal Raman spectroscopy and fluorescence spectroscopy
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共聚焦拉曼光谱和荧光光谱研究聚乙二醇化乳化剂作为渗透促进剂的皮肤渗透
DOI：
10.1016/j.ejpb.2021.04.027
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发表时间：
2021-06-02
影响因子：
4.9
通讯作者：
Lunter, Dominique Jasmin
中科院分区：
文献类型：
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作者：
Liu, Yali;Lunter, Dominique Jasmin
非离子乳化剂一直是皮肤分析领域的研究热点。为了发现它们在皮肤药物递送系统中作为渗透促进剂的作用，聚乙二醇（PEG）醚的聚乙二醇化乳化剂被靶向离体研究。通过常规胶带剥离法和共焦拉曼光谱（CRS）检测了它们在促进皮肤渗透方面的有效性。分别以黄绿素钠（Fluo-Na）和盐酸普鲁卡因为模型药物。从透皮量和透皮深度两个方面比较了两种药物的释药性能。基于两种分析的结果，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油醚（O2）更能促进药物的深部分布，尤其是PEG-20十六烷基醚（C20）的作用更明显。根据这项研究，它们的渗透增强性能似乎与它们对细胞间脂质的中断有关，这可以被认为是控制聚乙二醇化乳化剂作为渗透增强剂的能力的潜在机制。进一步的仪器比较突出了使用CRS作为皮肤渗透分析替代方法的益处。
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.