Sherertz E F, Sloan K B, McTiernan R G
Veterans Administration Medical Center (Research Service), Gainesville, Florida.
Arch Dermatol Res. 1990;282(7):463-8. doi: 10.1007/BF00402624.
A 2% commercial solution formulation of 5-fluorouracil (5-FU) was significantly better at delivering 5-FU than either a 1% or 5% solution. Among single component suspension formulations the highest transdermal delivery was obtained from the vehicle in which 5-FU was least soluble, isopropyl myristate (IPM), while changes in the total suspended concentration of 5-FU in propyleneglycol (PG) had no significant effect on transdermal delivery by those suspensions. A prodrug of 5-FU/IPM was significantly better at delivering 5-FU than any of the formulations. The trends in relative rates of delivery of 5-FU by the formulations and the prodrug were the same in skin of hairless mice and humans. The mouse skin was about ten times more permeable than the human skin. Second application studies to assess skin damage caused by the formulations also showed the same trend in skin of hairless mice and humans: all of the formulations caused some damage.
5-氟尿嘧啶（5-FU）的2%商用溶液制剂在递送5-FU方面明显优于1%或5%的溶液。在单一组分混悬剂制剂中，5-FU溶解度最低的载体肉豆蔻酸异丙酯（IPM）实现了最高的透皮递送，而丙二醇（PG）中5-FU总混悬浓度的变化对这些混悬剂的透皮递送没有显著影响。5-FU/IPM前药在递送5-FU方面明显优于任何一种制剂。制剂和前药递送5-FU的相对速率趋势在无毛小鼠和人类皮肤中是相同的。小鼠皮肤的渗透性约为人类皮肤的十倍。评估制剂引起的皮肤损伤的二次应用研究在无毛小鼠和人类皮肤中也显示出相同的趋势：所有制剂都会造成一些损伤。
