University of Vienna, Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Life Sciences, Althanstraße 14, 1090 Vienna, Austria.
Int J Pharm. 2012 Feb 28;423(2):535-42. doi: 10.1016/j.ijpharm.2011.11.037. Epub 2011 Dec 1.
Numerous reports on the enhancement effect of cyclodextrins (CDs) on the skin permeation of dermally applied drugs exist, the majority of which is based on in vitro diffusion cell studies. The specific experimental setup of such studies may skew the obtained results, which is rarely discussed in the context of CD studies. Thus, the aim of this work was to conduct a systematic in vitro investigation of the permeation enhancement potential of γ-CD on a steroidal drug from a nanoemulsion. The role of critical diffusion cell parameters such as the dose of application, occlusive conditions, the nature of the receptor medium and the skin thickness were investigated. The results showed that significantly enhanced skin permeation rates of fludrocortisone acetate were indeed caused by 1% (w/w) of γ-CD at both finite and infinite dose conditions. At 0.5% (w/w) of γ-CD, significant enhancement was only achieved at infinite dose application. Additional in vitro tape stripping experiments confirmed these tendencies, but the observed effects did not reach statistical significance. It may be concluded that the full permeation enhancement potential of the CD as observed in the Franz-cell setup can only be realised at infinite dose conditions while preserving the formulation structure.
有大量关于环糊精（CDs）对经皮应用药物皮肤渗透增强作用的报告，其中大多数基于体外扩散池研究。这些研究的特定实验设置可能会扭曲获得的结果，而这在 CD 研究中很少被讨论。因此，本工作的目的是对纳米乳中甾体药物的 γ-CD 的渗透增强潜力进行系统的体外研究。研究了关键扩散池参数的作用，如应用剂量、封闭条件、受体介质的性质和皮肤厚度。结果表明，在有限和无限剂量条件下，1%（w/w）的 γ-CD 确实显著提高了醋酸氟轻松的皮肤渗透速率。在 0.5%（w/w）的 γ-CD 下，仅在无限剂量应用时才观察到显著的增强。额外的体外胶带剥离实验证实了这些趋势，但观察到的效果没有达到统计学意义。可以得出结论，只有在无限剂量条件下并保持制剂结构，才能在 Franz 细胞装置中观察到 CD 的完全渗透增强潜力。
