School of Medicine, The University of Queensland, Princess Alexandra Hospital, Brisbane, Woolloongabba, Queensland, Australia.
J Pharm Sci. 2010 Feb;99(2):712-8. doi: 10.1002/jps.21856.
We examined uptake of the model therapeutic agent, minoxidil, into appendages, stratum corneum (SC), and through human skin, under the influence of different vehicles. Quantitative estimation of therapeutic drug deposition into all three areas has not previously been reported. Finite doses of minoxidil (2%, w/v) in formulations containing varying amounts of ethanol, propylene glycol (PG), and water (60:20:20, 80:20:0, and 0:80:20 by volume, respectively) were used. Minoxidil in SC (by tape stripping), appendages (by cyanoacrylate casting), and receptor fluid was determined by liquid scintillation counting. At early times (30 min, 2 h), ethanol-containing formulations (60:20:20 and 80:20:0) caused significantly greater minoxidil retention in SC and appendages, compared to the formulation lacking ethanol (0:80:20). A significant increase in minoxidil receptor penetration occurred with the PG-rich 0:80:20 formulation after 12 h. We showed that deposition of minoxidil into appendages, SC, and skin penetration into receptor fluid were similar in magnitude. Transport by the appendageal route is likely to be a key determinant of hair growth promotion by minoxidil.
我们研究了不同载体对模型治疗药物米诺地尔进入附属物、角质层（SC）和人体皮肤的影响。此前，尚未有报道对所有三个区域的治疗药物沉积进行定量评估。我们使用了含有不同量乙醇、丙二醇（PG）和水的米诺地尔（2%，w/v）制剂，其体积比分别为 60:20:20、80:20:0 和 0:80:20。通过液体闪烁计数法测定 SC（通过胶带剥离）、附属物（通过氰基丙烯酸酯铸型）和受体液中的米诺地尔含量。在早期（30 分钟，2 小时），与不含乙醇的制剂（0:80:20）相比，含有乙醇的制剂（60:20:20 和 80:20:0）导致 SC 和附属物中米诺地尔的保留量显著增加。12 小时后，富含 PG 的 0:80:20 制剂显著增加了米诺地尔受体的渗透。我们表明，米诺地尔进入附属物、SC 和皮肤渗透到受体液中的沉积量相似。附属物途径的输送可能是米诺地尔促进毛发生长的关键决定因素。
