Research Platform Characterisation of Drug Delivery Systems on Skin and Investigation of Involved Mechanisms, University of Vienna, Vienna 1090, Austria.
J Pharm Sci. 2013 Aug;102(8):2699-706. doi: 10.1002/jps.23646. Epub 2013 Jun 21.
The skin penetration of flufenamic acid (Fluf) and fluconazole (Fluc) from innovative natural microemulsions was investigated in tape-stripping experiments on pig ears. The formulations were based on the eudermic surfactants lecithin, sucrose laurate, alkylpolyglycoside or a mixture thereof. The quantification of the penetrated drug amounts was executed by (19) F nuclear magnetic resonance (NMR) in comparison with high-performance liquid chromatography (HPLC). The data obtained by the (19) F NMR method were confirmed by additional quantitative studies using HPLC. An excellent linear correlation was found for Fluf as well as for Fluc between (19) F NMR and HPLC data. This work presents a strategy outlining the use of (19) F NMR to selectively monitor the skin penetration routes of fluorinated compounds. Fluc penetrated generally well into the stratum corneum with the significantly highest amounts from the sucrose laurate microemulsion on the tape strips 1-5. Similarly, the highest amounts of penetrated Fluf could be observed from the formulation based on sucrose laurate. In addition, NMR self-diffusion studies were conducted and revealed a bicontinuous microstructure of the investigated microemulsions. The skin penetration results are in good agreement with the obtained (19) F NMR self-diffusion coefficients of the active compounds in the microemulsion systems.
在猪耳的胶带剥离实验中研究了创新型天然微乳液中氟芬酸（Fluf）和氟康唑（Fluc）的皮肤渗透。这些配方基于角质层友好型表面活性剂卵磷脂、月桂酰蔗糖、烷基糖苷或它们的混合物。与高效液相色谱（HPLC）相比，通过（19）F 核磁共振（NMR）定量测定穿透的药物量。（19）F NMR 方法获得的数据通过使用 HPLC 进行的额外定量研究得到证实。Fluf 和 Fluc 之间均发现（19）F NMR 和 HPLC 数据之间存在极好的线性相关性。这项工作提出了一种策略，概述了使用（19）F NMR 选择性监测氟化化合物的皮肤渗透途径。Fluc 通常很好地渗透到角质层中，在胶带 1-5 上来自月桂酰蔗糖微乳液的量显著最高。同样，来自基于月桂酰蔗糖的制剂的穿透 Fluf 的量最高。此外，还进行了 NMR 自扩散研究，揭示了所研究的微乳液的双连续微观结构。皮肤渗透结果与微乳液系统中活性化合物的获得的（19）F NMR 自扩散系数非常吻合。
