INVITRO EVALUATION OF A SERIES OF AZONE ANALOGS AS DERMAL PENETRATIONENHANCERS .1.

The influence of a series of Azone analogs on the percutaneous penetra tion of a lipophilic model drug (hydrocortisone-21-acetate) across hai rless mouse skin has been investigated. Methods of synthesis of these novel compounds are also described. Permeability studies utilized vert ical non-occluded Franz cells at 37-degrees-C and propylene glycol as the vehicle for the drug. Enhancers were applied one h prior to drug t reatment in the same vehicle. Three enhancers were applied at their ma ximum saturation solubilities in propylene glycol, the rest of the com pounds at 0.4 M. Enhancement ratios were calculated for flux, 24 h dif fusion cell receptor concentrations, and full-thickness skin total ste roid contents. All enhancers were found to increase permeation paramet ers to a greater or lesser extent over control. A few compounds were f ound to be more effective than Azone in increasing these parameters; p articularly skin retention of the model drug.