脂肪酸作为化学渗透增强剂的效率：作用机制和结构增强关系。
Efficiency of fatty acids as chemical penetration enhancers: mechanisms and structure enhancement relationship.
机构信息
Division of Pharmaceutical Sciences, College of Pharmacy, University of Cincinnati, 3225 Eden Avenue, Rm 136 HPB, Cincinnati, Ohio 45267-0004, USA.
出版信息
Pharm Res. 2010 Jan;27(1):115-25. doi: 10.1007/s11095-009-9985-0. Epub 2009 Nov 13.
PURPOSE
The present study evaluated the effects of fatty acids commonly present in cosmetic and topical formulations on permeation enhancement across human epidermal membrane (HEM) lipoidal pathway when the fatty acids saturated the SC lipid domain without cosolvents (Emax).
METHODS
HEM was treated with neat fatty acids or fatty acid suspensions to determine Emax. A volatile solvent system was used to deposit fatty acids on HEM surface to compare fatty acid enhancer efficiency in topical volatile formulations with Emax. To elucidate permeation enhancement mechanism(s), estradiol (E2beta) uptake into fatty acid-treated SC lipid domain was determined.
RESULTS
Emax of fatty acids was shown to increase with their octanol solubilities and decrease with their lipophilicities, similar to our previous findings with other enhancers. Emax of solid fatty acids was shown to depend on their melting points, an important parameter to the effectiveness of the enhancers. The E2beta uptake results suggest that enhancer-induced permeation enhancement across HEM is related to enhanced permeant partitioning into the SC lipid domain.
CONCLUSIONS
The results suggest Emax as a model for studying the permeation enhancement effect of the fatty acids and their structure enhancement relationship.
目的
本研究评估了化妆品和局部制剂中常见脂肪酸在脂肪酸饱和角质层脂质区域（Emax）而无需共溶剂的情况下对经皮渗透的影响。
方法
采用纯脂肪酸或脂肪酸混悬液处理人表皮膜（HEM）以确定 Emax。采用挥发性溶剂系统将脂肪酸沉积在 HEM 表面，以比较 Emax 下局部挥发性制剂中脂肪酸增强剂的效率。为阐明渗透增强机制，测定了进入脂肪酸处理的角质层脂质区域的雌二醇（E2beta）摄取量。
结果
与我们之前对其他增强剂的研究结果相似，脂肪酸的 Emax 随其辛醇溶解度的增加而增加，随其亲脂性的降低而降低。固态脂肪酸的 Emax 取决于其熔点，这是增强剂有效性的一个重要参数。E2beta 摄取结果表明，增强剂诱导的 HEM 经皮渗透增强与进入角质层脂质区域的透皮物分配增强有关。
结论
结果表明，Emax 可作为研究脂肪酸渗透增强作用及其结构增强关系的模型。
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