TRANSDERMAL AND DERMAL ENHANCING ACTIVITY OF PYRROLIDINONES IN HAIRLESS MOUSE SKIN

The transdermal penetration-enhancing abilities of 16 pyrrolidinones w ere tested against the model drug hydrocortisone using a hairless mous e skin model in vitro. Skins were pretreated for I h with the enhancer in propylene glycol before application of the drug also in propylene glycol. Enhancement ratios (ER) were calculated for permeability coeff icient (P), 24-h receptor concentration (Q(24)), and skin content of d rug (SC) and compared to control values (no enhancer present). N-Dodec yl-2-pyrrolidinone and 2-pyrrolidinone-1-acetic acid dodecyl ester wer e found to produce the greatest enhancement for all the parameters cal culated with ER for Q(24) of 23.11 and 11.68, respectively. These same enhancers also produced high ERs for P with 42.95 and 41.07, respecti vely. These values exceed Atone's enhancement ratios for the same para meters and hence these enhancers are candidates for further developmen t as penetration enhancers. (C) 1997 Elsevier Science B.V.