Nguyen Hiep X, Puri Ashana, Banga Ajay K
Department of Pharmaceutical Sciences, College of Pharmacy, Mercer University, Atlanta, GA 30341, United States.
Department of Pharmaceutical Sciences, College of Pharmacy, Mercer University, Atlanta, GA 30341, United States.
Int J Pharm. 2017 Mar 15;519(1-2):22-33. doi: 10.1016/j.ijpharm.2017.01.007. Epub 2017 Jan 3.
Rubbing a topical formulation on skin is generally assumed to enhance drug penetration. The aim of this study was to demonstrate different techniques such as using glass rod, rheometer, and gloved finger for rubbing a 2% salicylic acid gel on skin and investigate their effect on in vitro permeation of salicylic acid through dermatomed porcine ear skin. The studies included evaluation of the gel's rheological properties, gel distribution on skin surface, in vitro permeability, drug distribution in skin, skin extraction recovery, and mass balance. Rubbing with a gloved finger resulted in a uniform gel layer with a thickness of 49.61±15.33μm on the skin surface. No significant difference between the different test groups was observed in terms of the cumulative amount of drug that permeated in 24h (p>0.05). Drug levels in stratum corneum, epidermis, and dermis were also analyzed. Rubbing with gloved finger delivered significantly higher amount of drug into the skin layers as compared to other test groups (p<0.05). Amount of drug extracted from skin was reliably correlated to the actual drug levels in skin (R=0.99). Considering drug amounts in different compartments, mass balance ranged from 75.86±2.90% to 80.44±2.99%.
通常认为在皮肤上涂抹局部用制剂可增强药物渗透。本研究的目的是展示不同的涂抹技术，如使用玻璃棒、流变仪和戴手套的手指在皮肤上涂抹2%水杨酸凝胶，并研究它们对水杨酸通过去角质猪耳皮肤的体外渗透的影响。研究内容包括评估凝胶的流变学性质、凝胶在皮肤表面的分布、体外渗透性、药物在皮肤中的分布、皮肤提取回收率和质量平衡。用戴手套的手指涂抹后，皮肤表面形成了一层均匀的凝胶层，厚度为49.61±15.33μm。在24小时内渗透的药物累积量方面，不同测试组之间未观察到显著差异（p>0.05）。还分析了角质层、表皮和真皮中的药物水平。与其他测试组相比，用戴手套的手指涂抹将显著更多的药物输送到皮肤层中（p<0.05）。从皮肤中提取的药物量与皮肤中的实际药物水平具有可靠的相关性（R=0.99）。考虑到不同隔室中的药物量，质量平衡范围为75.86±2.90%至80.44±2.99%。
