Pyrrolidones as penetration enhancers

Abstract

Pyrrolidines are not widely researched in the recent years as percutaneous penetration enhancers. The toxicity and skin irritancy of these enhancers may be the reason that these enhancers are not studied further. N-methyl-2-pyrrolidone (NMP) and its combination with other solvents such as isopropyl myristate (IPM) are researched in recent years for their synergistic enhancements in the percutaneous absorption of drugs. Pyrrolidones act as penetration enhancers due to their effects on the intercellular lipid bilayers in the stratum corneum. These enhancers penetrate into this region in such amounts that they alter the solubilizing ability of this site, thereby promoting drug partition into the skin. NMP is also known to form hydrogen bonds with basic drugs and cotransport the penetrant across the skin.