Enhancing effect of combining two pyrrolidone vehicles on transdermal drug delivery.
The enhancing effect of combining 1-methyl-2-pyrrolidone (MP) and 1-lauryl-2-pyrrolidone (LP) as the vehicles for transdermal penetration of phenolsulphonphthalein (phenol red) has been investigated by using an in-vitro technique with excised rat skin. LP had a higher enhancing effect on the penetration of phenol red than MP, but there was a long lag time before steady-state penetration was attained. A potent effect with a shorter lag time was obtained when MP and LP were used together. This potentiation was maintained when the concentration of MP was decreased by 95%. The combined vehicle also enhanced the skin accumulation of phenol red. MP promoted the rapid penetration of LP into the skin and potentiated the enhancing effect of LP on the penetration of phenol red and thereby shortened the lag time. The combined vehicle also enhanced the penetration of the hydrophilic anticancer agent, 5-fluorouracil.
Sasaki
H
H
Faculty of Pharmaceutical Sciences, Nagasaki University, Japan.
Kojima
M
M
Nakamura
J
J
Shibasaki
J
J
D000279:Administration, Cutaneous; D000818:Animals; D002851:Chromatography, High Pressure Liquid; D005472:Fluorouracil / Q000493:pharmacokinetics; D066298:In Vitro Techniques; D008297:Male; D014677:Pharmaceutical Vehicles; D010637:Phenolsulfonphthalein / Q000493:pharmacokinetics; D011760:Pyrrolidinones / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D012869:Skin Absorption / Q000187:drug effects*
D014677:Pharmaceutical Vehicles; D011760:Pyrrolidinones; C065136:1-lauryl-2-pyrrolidone; D010637:Phenolsulfonphthalein; C038678:N-methylpyrrolidone; D005472:Fluorouracil