A transdermal preparation containing ketoprofen was developed using O/W mic
roemulsion system. Of the oils tested, oleic acid was chosen as the oil pha
se of the microemulsion, as it showed a good solubilizing capacity and exce
llent skin permeation rate of the drug. Pseudoternary phase diagrams were c
onstructed to obtain the concentration range of oil, surfactant and cosurfa
ctant for microemulsion formation, and the effect or these additives on ski
n permeation of ketoprofen was evaluated with excised rat skins. The optimu
m formulation of the microemulsion consisted of 3% ketoprofen, 6% oleic aci
d, 30% Labrasol/Cremophor RH 40 (1:1) and water. Terpenes were added to the
microemulsion at the level of 5% and their effect on the skin permeation o
f ketoprofen from the microemulsion was evaluated. Of the four terpenes use
d, only limonene resulted in a powerful enhancing activity (3-fold increase
over control). (C) 2001 Elsevier Science B.V. All rights reserved.