The percutaneous absorption of a fentanyl (FEN)-patch is affected by various external factors including the volume of sebum secretion, which causes changes in the skin surface environment. In this study, we prepared a lard-based sebum-like secretion (SLS), and applied it to investigate the effect of different skin surface conditions on the drug penetration of a FEN-patch. In vitro work to test drug release using the Franz diffusion cell indicated that drug release was significantly suppressed by treatment with 5% SLS, which is equivalent to the amount of daily human sebum secretion. Conversely, in ex vivo experiments using rat skin, the amount of FEN that accumulated in the skin tissue of the 5% SLS-treated rats was higher in comparison with the non-SLS treated group. Furthermore, in vivo experiments indicated that the plasma FEN concentration in rats treated with the FEN-patch was significantly increased by treatment with 5% SLS. These results suggest that the sebum affected the release, accumulation, and absorption of FEN from the FEN-patch, and the FEN concentration in the blood was reflected by the balance of the suppression of drug release and the enhancement of drug accumulation in the skin with SLS.

芬太尼（FEN）贴剂的经皮吸收受到各种外部因素的影响，其中包括皮脂分泌量，这会引起皮肤表面环境的变化。在这项研究中，我们准备了猪油样皮脂样分泌物（SLS），并将其用于研究不同皮肤表面状况对FEN贴剂药物渗透的影响。使用Franz扩散池测试药物释放的体外研究表明，用5％SLS处理可显着抑制药物释放，这相当于人类日常皮脂分泌量。相反，在使用大鼠皮肤的离体实验中，与未经SLS处理的组相比，在5％SLS处理的大鼠的皮肤组织中积累的FEN量更高。此外，体内实验表明，用5％SLS处理后，用FEN贴片处理的大鼠血浆FEN浓度显着增加。这些结果表明皮脂影响FEN贴片中FEN的释放，积累和吸收，血液中FEN的浓度通过抑制药物释放和增加皮肤中药物积累的平衡来反映。 SLS。