Concentration Dependency in Nicotine Skin Penetration Flux from Aqueous Solutions Reflects Vehicle Induced Changes in Nicotine Stratum Corneum Retention
Concentration Dependency in Nicotine Skin Penetration Flux from Aqueous Solutions Reflects Vehicle Induced Changes in Nicotine Stratum Corneum Retention
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DOI：
10.1007/s11095-013-1256-4
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发表时间：
2014-06-01
影响因子：
3.7
通讯作者：
Roberts, Michael S.
中科院分区：
文献类型：
--
作者：
Kuswahyuning, Rina;Roberts, Michael S.
本研究采用Franz扩散池测定了一系列尼古丁水溶液中尼古丁通过人体表皮的稳态通量及其在角质层中的含量，并采用高效液相色谱法（HPLC）对尼古丁进行了分析。尼古丁的热力学活性在各种解决方案估计从其部分蒸汽压和角质层水合作用测定使用角质计。保留在角质层中的尼古丁量是根据在单个角质层胶带条中发现的尼古丁量和D-Squame确定的每个条带的重量来估计的。观察到的尼古丁穿过人表皮的稳态通量被发现显示出对尼古丁浓度的抛物线依赖性，通量与其热力学活性成比例，直到浓度为48%w/w。尼古丁在角质层中的保留表现出类似的浓度依赖性，而尼古丁在角质层中的扩散率似乎与浓度无关。反过来，这种保留可以通过角质层水合程度、应用溶液中的尼古丁浓度和皮肤中水的体积来估计。尼古丁皮肤通量对其浓度的非线性依赖性是由于脱水引起的角质层保留在较高浓度下的减少，而不是脱水引起的角质层中尼古丁扩散率的变化。
This study sought to understand the mechanism by which the steady state flux of nicotine across the human skin from aqueous solutions is markedly decreased at higher nicotine concentrations.Nicotine's steady state flux through human epidermis and its amount in the stratum corneum for a range of aqueous nicotine solutions was determined using Franz diffusion cells, with the nicotine analysed by high performance liquid chromatography (HPLC). Nicotine's thermodynamic activity in the various solutions was estimated from its partial vapour pressure and stratum corneum hydration was determined using a corneometer. The amount of nicotine retained in the stratum corneum was estimated from the nicotine amount found in individual stratum corneum tape strips and a D-Squame determined weight for each strip.The observed steady state flux of nicotine across human epidermis was found to show a parabolic dependence on nicotine concentration, with the flux proportional to its thermodynamic activity up to a concentration of 48% w/w. The nicotine retention in the stratum corneum showed a similar dependency on concentration whereas the diffusivity of nicotine in the stratum corneum appeared to be concentration independent. This retention, in turn, could be estimated from the extent of stratum corneum hydration and the nicotine concentration in the applied solution and volume of water in the skin.Nonlinear dependency of nicotine skin flux on its concentration results from a dehydration induced decrease in its stratum corneum retention at higher concentration and not dehydration induced changes nicotine diffusivity in the stratum corneum.