| abstract |
A novel positively charged prodrug of ibuprofen represented by formula (1) was synthesized. The positively charged amino groups of these prodrugs not only greatly increase the solubility of the drug, but also bind to the negative charge on the membrane phosphate head group, pushing the prodrug into the cytosol. The prodrug, diethylaminoethyl 2- (p-isobutylphenyl) propionate acetate, diffuses through human skin ˜250 times faster than ibuprofen itself and ˜125 times faster than ethyl 2- (p-isobutylphenyl) propionate. Prodrugs can be used pharmaceutically not only for oral administration but also transdermally to treat ibuprofen-treatable conditions in humans or animals, avoiding the side effects of most ibuprofen. A controlled transdermal delivery system for prodrugs allows ibuprofen to continually reach optimal therapeutic blood levels, increase efficacy, and reduce ibuprofen side effects. |