Loftsson T, Somogyi G, Bodor N
Acta Pharm Nord. 1989;1(5):279-86.
Five choline esters, lauroylcholine, myristoylcholine, palmitoylcholine, stearoylcholine and oleoylcholine, were evaluated as skin penetration enhancers by testing their effects on the penetration of six drugs, acyclovir, 17 beta-estradiol, hydrocortisone, nitroglycerin, all-trans-retinoic acid and trifluorothymidine, across hairless mouse skin in vitro and comparing the results to those obtained with oleic acid. The results show that the transdermal delivery of the drugs tested from propylene glycol vehicle systems, can be significantly increased by adding small amounts of choline esters and/or oleic acid to the vehicle. Lauroylcholine was a better enhancer than oleic acid for the transdermal delivery of 17 beta-estradiol and, in mixtures, lauroylcholine and oleic acid acted as synergists giving larger enhancement of the transdermal delivery of nitroglycerin and acyclovir than when used separately.
通过测试五种胆碱酯（月桂酰胆碱、肉豆蔻酰胆碱、棕榈酰胆碱、硬脂酰胆碱和油酰胆碱）对六种药物（阿昔洛韦、17β-雌二醇、氢化可的松、硝酸甘油、全反式维甲酸和三氟胸苷）经体外无毛小鼠皮肤渗透的影响，并将结果与用油酸获得的结果进行比较，来评估它们作为皮肤渗透促进剂的效果。结果表明，通过向丙二醇载体系统中添加少量胆碱酯和/或油酸，所测试药物从该载体系统的透皮递送可显著增加。对于17β-雌二醇的透皮递送，月桂酰胆碱是比油酸更好的促进剂，并且在混合物中，月桂酰胆碱和油酸起协同作用，相比于单独使用时，能更大程度地促进硝酸甘油和阿昔洛韦的透皮递送。
