Abe Akinari, Suzuki Hiromichi, Amagai Sayaka, Saito Miyuki, Itakura Shoko, Todo Hiroaki, Sugibayashi Kenji
Graduate School of Pharmaceutical Sciences, Josai University.
Research & Development Headquarters Self-Medication, Taisho Pharmaceutical Co., Ltd.
Chem Pharm Bull (Tokyo). 2021;69(8):806-810. doi: 10.1248/cpb.c21-00181.
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.
研究了擦涂对亲水性药物咖啡因（CAF）和亲脂性药物杜鹃醇（RD）从乳液和乳膏中经皮渗透的影响。擦涂作用可显著增加CAF的经皮渗透，且与制剂类型无关。此外，皮肤渗透增强效果受擦涂方向影响：与沿头发生长方向擦涂以及在皮肤上以圆周方式擦涂相比，逆头发生长方向擦涂时渗透率最高。另一方面，无论制剂类型如何，擦涂对RD的经皮渗透均未观察到增强作用。擦涂及随后的皮肤拉伸导致毛囊漏斗口尺寸的变化可能与CAF较高的经皮渗透有关。相比之下，RD在角质层中的高分布可能是擦涂作用未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。
