渗透
亲脂性
化学
溶解度
膜
色谱法
体外
人体皮肤
乙醇
磁导率
牛血清白蛋白
生物物理学
立体化学
生物化学
有机化学
生物
遗传学
作者
Azadeh Alinaghi,Ana S. Macedo,Hanumanth Srikanth Cheruvu,Amy Holmes,Michael S. Roberts
标识
DOI:10.1016/j.ijpharm.2022.122114
摘要
This study examined a number of factors that can impact the outcomes of in vitro human epidermal permeation coefficients for aliphatic alcohols and steroids, including receptor phase composition and study conditions. We determined experimentally the solubilities and IVPT permeation of a homologous series of 14C labeled aliphatic alcohols (ethanol, propanol, pentanol, heptanol, octanol and decanol) in different receptor fluids as recommended by Organisation Economic Co-operation and Development (OECD). We used human epidermal membranes at 25 °C and phosphate-buffered saline (PBS), 2 %w/v bovine serum albumin (2 %w/v BSA), 50 %w/v ethanol and 0.1, 2 and 6 %w/v Oleth-20 receptor phases. We also explored and confirmed the discrepancies between in vitro human epidermal permeability coefficients (kp) and diffusion lag times for steroids from Scheuplein's group with our own work and that of others. The main reason for the observed differences is not clear but is likely to be multifactorial, including the effects of diffusion cell design, receptor phase solubility, unstirred receptor phase effects, epidermal membrane hydration, diffusion cell configuration, transport through appendageal pathways and steroid lipophilicity. We conclude with a summary of experimental conditions that should be considered in undertaking IVPT studies.
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