Yang J J, Roy T A, Mackerer C R
Toxicol Ind Health. 1986 Dec;2(4):409-16. doi: 10.1177/074823378600200404.
Percutaneous absorption of 14C-labeled benzo[a]pyrene (BaP) was studied in five-day in vivo and in vitro experiments with female Sprague-Dawley rats following single topical doses of 9-10 micrograms/cm2. The in vivo percutaneous absorption was measured by the presence of 14C radioactivity in urine, feces and tissues. In vitro percutaneous absorption was measured with excised (non-viable) skin in Franz-type diffusion cells. Several modifications of standard diffusion cell techniques which are known to enhance the transport of lipophilic compounds were evaluated. In vitro penetration was determined by directly measuring the level of 14C radioactivity in the receptor fluid. BaP was observed to readily penetrate in vivo with a total of 46.2% (n = 4, SD = 3.4%) of the applied dose being absorbed over five days. In in vitro experiments using an approximately 350 micronthick skin section and normal saline receptor solution, only 2.1% of the applied BaP diffused into the receptor fluid over five days. In in vitro experiments using full-thickness skin and a 6% solution of nonionic surfactant receptor fluid, 28.0% of the applied BaP diffused into the receptor fluid over five days. When both an approximately 350 microns-thick skin section and a 6% surfactant receptor solution were used in vitro, 49.9% (n = 4, SD = 3.1%) of the BaP dose was found in the receptor fluid after five days. The results show that the modified in vitro method is suitable for studying percutaneous absorption of lipophilic compounds such as BaP.
采用雌性斯普拉格-道利大鼠，以9 - 10微克/平方厘米的单次局部剂量，进行了为期五天的体内和体外实验，研究了经皮吸收14C标记的苯并[a]芘（BaP）的情况。通过尿液、粪便和组织中14C放射性的存在来测量体内经皮吸收情况。在弗兰兹型扩散池中，用切除的（无活力的）皮肤测量体外经皮吸收情况。评估了几种已知能增强亲脂性化合物转运的标准扩散池技术的改进方法。通过直接测量受体液中14C放射性水平来确定体外渗透情况。观察到BaP在体内易于渗透，在五天内共吸收了46.2%（n = 4，标准差 = 3.4%）的给药剂量。在体外实验中，使用约350微米厚的皮肤切片和生理盐水受体液，五天内只有2.1%的给药BaP扩散到受体液中。在体外实验中，使用全层皮肤和6%的非离子表面活性剂受体液，五天内28.0%的给药BaP扩散到受体液中。当在体外同时使用约350微米厚的皮肤切片和6%的表面活性剂受体液时，五天后在受体液中发现49.9%（n = 4，标准差 = 3.1%）的BaP剂量。结果表明，改进后的体外方法适用于研究BaP等亲脂性化合物的经皮吸收。
