Effect of 1-alkyl- or 1-alkenylazacycloalkanone derivatives on penetration of mitomycin C through rat skin.

(3, 7, 11-trimethyldodecyl ) azacycloheptan-2-one (7FS), l-geranylgeranylazacycloheptan-2-one (7GGU), and 1-geranylgeranylazacyclohexan-2-one (6GGU), on percutaneous penetration of mitomycin C (MMC) through rat skin in vitro were investigated in comparison with those of 1farnesylazacycloheptan-2-one (7FU) and 1-dodecylazacycloheptan-2-one (Azone) . In an in vitro diffusion experiment, 6GU, 7GS, 7FU, 7FS, 7GGU, 6GGU, and Azone significantly enhanced MMC penetration through rat skin compared with the control. The size of the azacyclo ring had little effect on the potency of these penetration enhancers. On the other hand, the changes in the length of the hydrophobic chain resulted in some variation in the activity of these compounds . Azone and 7FU, which have a hydrophobic chain of length of twelve carbons, were the most effective among enhancers with an azacycloheptanone ring, and 7GGU, with the longest hydro-