College of Pharmacy, Taipei Medical University, 250 Wu-Hsing Street, Taipei 110, Taiwan, ROC.
Spectrochim Acta A Mol Biomol Spectrosc. 2009 Oct 15;74(3):695-703. doi: 10.1016/j.saa.2009.08.001. Epub 2009 Aug 8.
Tocopheryl polyethylene glycol succinate (TPGS) is a water-soluble derivative of natural source of vitamin E, which possesses a dual nature of lipophilicity and hydrophilicity, similar to a surface-active agent. The penetration enhancement of estradiol by an ethanol and TPGS cosolvent system (EtOH/TPGS) has been confirmed. In this study, the correlation of the penetration enhancement with the influence of the EtOH/TPGS cosolvent system on biophysical changes of the stratum corneum (SC) as examined by Fourier transformation infrared spectrometry differential scanning calorimetry (FTIR/DSC) was investigated. Thermotropic changes in the asymmetrical and symmetrical C-H stretching of hydrocarbon chains of lipids, and amide I and II bands that characterize the protein structure of the SC treated with different concentrations of the EtOH/TPGS cosolvent were examined in this investigation. Results demonstrated that a strong correlation of the influence on biophysical changes of the SC treated with the EtOH/TPGS cosolvent system with the penetration enhancement of estradiol by the corresponding cosolvent system was not evident. It was concluded that the incorporation of TPGS in the cosolvent system seemed only to have insignificantly modified the structural features of the SC. It was not obvious that the penetrant had encountered these modifications resulting in an improvement in the penetration of estradiol by TPGS.
生育酚聚乙二醇琥珀酸酯（TPGS）是维生素 E 的天然来源的水溶性衍生物，具有亲脂性和亲水性的双重性质，类似于表面活性剂。已经证实，乙醇和 TPGS 共溶剂系统（EtOH/TPGS）可增强雌二醇的渗透。在这项研究中，通过傅里叶变换红外光谱差示扫描量热法（FTIR/DSC）研究了渗透增强与 EtOH/TPGS 共溶剂系统对角质层（SC）生物物理变化的影响之间的相关性。在这项研究中，检查了用不同浓度的 EtOH/TPGS 共溶剂处理的脂质不对称和对称 C-H 伸缩振动以及酰胺 I 和 II 带的热变性，这些带特征是 SC 的蛋白质结构。结果表明，用 EtOH/TPGS 共溶剂系统处理 SC 的生物物理变化的影响与相应共溶剂系统对雌二醇渗透增强之间的强相关性并不明显。结论是，共溶剂系统中 TPGS 的掺入似乎仅略微改变了 SC 的结构特征。渗透物是否遇到这些变化导致 TPGS 对雌二醇的渗透增强尚不清楚。
