Exp Dermatol. 2012 Mar;21(3):226-8. doi: 10.1111/j.1600-0625.2011.01429.x.
The aim was to investigate the feasibility of using iontophoresis for the cutaneous delivery of the E-selectin antagonist CGP69669A, a sialyl Lewis(x) -glycomimetic with potential activity against inflammatory skin diseases. The effects of current density and formulation on iontophoretic transport were evaluated in porcine and human skin in vitro. Cumulative permeation of CGP69669A increased with current density (69.73±9.51, 113.97±26.80 and 160.44±13.79μg/cm(2) at 0.1, 0.3 and 0.5mA/cm(2) , respectively) and drug concentration (37.42±13.13, 78.96±23.13 and 160.44±13.79μg/cm(2) , at 1, 3 and 5mg/ml, respectively). In contrast, passive delivery was negligible. Although permeation from a 2% hydroxyethyl cellulose gel was lower than that from aqueous solution, skin deposition - more relevant for the local treatment of dermatological conditions - was 3-fold higher. The results demonstrated that although CGP69669A cannot be delivered passively into the skin it is an excellent candidate for transdermal iontophoresis, a technique that is ideally suited to the delivery of glycomimetics.
目的在于研究电渗透法用于 E-选择素拮抗剂 CGP69669A（一种具有抗炎症性皮肤病活性的唾液酸 Lewis(x)-糖模拟物）经皮给药的可行性。在猪和人体皮肤的体外模型中，评估了电流密度和配方对电渗透传输的影响。CGP69669A 的累积渗透量随电流密度（分别为 0.1、0.3 和 0.5mA/cm²时为 69.73±9.51、113.97±26.80 和 160.44±13.79μg/cm²）和药物浓度（分别为 1、3 和 5mg/ml 时为 37.42±13.13、78.96±23.13 和 160.44±13.79μg/cm²）增加。相比之下，被动渗透可以忽略不计。尽管来自 2%羟乙基纤维素凝胶的渗透低于水溶液，但皮肤沉积（更适用于皮肤病局部治疗）是其 3 倍。结果表明，尽管 CGP69669A 不能经皮被动给药，但它是经皮电渗透的极佳候选药物，电渗透技术非常适合糖模拟物的传递。
