Effect of rubbing application on the skin permeation of a hydrophilic drug caffeine (CAF) and lipophilic drug rhododendrol (RD) from lotion and cream were investigated. Skin permeation of CAF was markedly increased by rubbing action independent of the formulation type. In addition, the skin penetration-enhancement effect was affected by the rubbing direction: rubbing application against the direction of hair growth showed the highest permeation compared with rubbing applications along the direction of hair growth and in a circular pattern on the skin. On the other hand, no enhancement effect was observed by the rubbing actions on the skin permeation of RD, regardless of formulation type. Change in the infundibula orifice size of hair follicles by the rubbing and following skin stretching may be related to the higher skin permeation for CAF. In contrast, high RD distribution into the stratum corneum may be a reason why no enhancement effect was observed by the rubbing action. These results can be helpful to predict safety and effectiveness of topically applied formulations.

研究了摩擦对乳液和乳膏中亲水性药物咖啡因 (CAF) 和亲脂性药物杜鹃花 (RD) 的皮肤渗透的影响。与配方类型无关的摩擦作用显着增加了 CAF 的皮肤渗透。此外，皮肤渗透增强效果受摩擦方向的影响：与毛发生长方向摩擦应用相比，与毛发生长方向摩擦应用相比，在皮肤上以圆形图案摩擦应用表现出最高的渗透。另一方面，无论配方类型如何，都没有观察到摩擦作用对 RD 皮肤渗透的增强作用。摩擦和皮肤拉伸后毛囊漏斗口大小的变化可能与 CAF 较高的皮肤渗透有关。相反，进入角质层的高RD分布可能是摩擦作用没有观察到增强效果的原因。这些结果有助于预测局部应用制剂的安全性和有效性。