Department of Pharmaceutical Technology, Faculty of Pharmacy, Istanbul University, Istanbul 34116, Turkey.
Molecules. 2013 May 10;18(5):5455-71. doi: 10.3390/molecules18055455.
The aim of this study was to develop novel transdermal films of ondansetron HCl with high molecular weight chitosan as matrix polymer and 2-(2-ethoxy-ethoxy) ethanol (Transcutol®) as plasticizer. In this context, firstly the physicochemical properties of gels used to formulate transdermal films were characterized and, physicochemical properties and bioadhesiveness of the transdermal films prepared with chitosan gels were assessed. The impact of three different types of terpenes, namely limonene, nerolidol and eucalyptol on in vitro skin permeation of ondansetron from transdermal films were also examined. ATR-FTIR measurements were performed to investigate the effects of the chitosan film formulations on in vitro conformational order of stratum corneum intercellular lipids after 24 h permeation study. The results showed that the chitosan gels consisting of Transcutol® as plasticizer and terpenes as penetration enhancer may be used to prepare transdermal films of ondansetron due to the good mechanical properties and bioadhesiveness of the transdermal films. Eucalyptol (1%) showed higher permeation enhancer effect than the other terpenes and control. ATR-FTIR data confirmed that finding in which eucalyptol induced a blue shift in the both CH₂ asymmetric and symmetric absorbance peak positions indicating increased lipid fluidity of stratum corneum.
本研究旨在开发新型盐酸昂丹司琼透皮贴剂，以高分子量壳聚糖为基质聚合物，2-(2-乙氧基乙氧基)乙醇（Transcutol®）为增塑剂。在这方面，首先对用于制备透皮贴剂的凝胶的理化性质进行了表征，并评估了用壳聚糖凝胶制备的透皮贴剂的理化性质和生物黏附性。还考察了三种不同类型的萜烯，即柠檬烯、橙花叔醇和桉油醇对透皮贴剂中昂丹司琼体外皮肤渗透的影响。ATR-FTIR 测量用于研究在体外渗透研究 24 小时后，壳聚糖膜配方对角质层细胞间脂质体外构象有序性的影响。结果表明，由于透皮贴剂具有良好的机械性能和生物黏附性，因此包含 Transcutol®作为增塑剂和萜烯作为渗透增强剂的壳聚糖凝胶可用于制备盐酸昂丹司琼透皮贴剂。桉油醇（1%）的渗透增强效果优于其他萜烯和对照。ATR-FTIR 数据证实了这一发现，即桉油醇诱导 CH₂不对称和对称吸收峰位置的蓝移，表明角质层的脂质流动性增加。
