Influence of drug lipophilicity on terpenes as transdermal penetration enhancers.

摘要: Percutaneous absorption-enhancing effects on the skin of hairless mice 11 monoterpenes [1, (+)-limonene; 2, (-)-menthone; 3, (+)-terpinen-4-ol; 4, alpha-terpineol; 5, 1,8-cineole; 6, (+)-carvone; 7, (-)-verbenone; 8, (-)-fenchone; 9, p-cymene; 10, (+)-neomenthol; and 11, geraniol] were investigated using three different model drugs (caffeine, hydrocortisone, triamcinolone acetonide [TA]) with varying lipophilicities. Terpenes applied at 0.4 M in propylene glycol (PG) to mouse skin. The as suspensions PG 1 hr following enhancer pretreatment. combination terpenes provided significant enhancement permeation caffeine through most active compounds 10 increased by between 13-fold 16-fold. also enhanced delivery but not great an extent. 3 4 3.9-fold 5-fold. examined did significantly increase TA. compound only 2.5-fold, while next 6 1.7-fold. Overall, these results indicate that can transdermal penetration hydrophilic drug polar steroid hydrocortisone.