Effect of different penetration enhancers on diclofenac permeation across horse skin.
Diclofenac is a hydrophilic non-steroidal anti-inflammatory drug widely used in humans and animals. Previous reports have shown that this compound has low percutaneous absorption in horses. The effect of five penetration enhancers (10% urea, 15% and 20% oleic acid and 5% and 10% d-limonene) on the percutaneous absorption of diclofenac diethylamine through horse skin was evaluated in vitro using Franz-type diffusion cells. All tested penetration enhancers induced a significant increase in diclofenac diethylamine permeation, with limonene showing the highest enhancing effect at the lowest concentration (5%) applied. The presence of the permeation enhancers did not affect lag-time. This is the first in vitro study of the effects of penetration enhancers on transdermal permeation of diclofenac diethylamine across horse skin. The results suggested that urea, limonene and 5% oleic acid were useful for enhancing the transdermal absorption of diclofenac diethylamine and may assist in the development of a transdermal formulation of diclofenac diethylamine for use in horses.
Ferrante
M
M
Cátedra de Farmacología, Facultad de Ciencias Veterinarias, Universidad Nacional de La Plata, Calle 60 y 118, cc 296 (1900), La Plata, CONICET, Argentina.
Andreeta
A
A
Landoni
M F
MF
D000279:Administration, Cutaneous; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000493:pharmacokinetics*; D053138:Cyclohexenes / Q000494:pharmacology; D004008:Diclofenac / Q000008:administration & dosage / Q000493:pharmacokinetics*; D004305:Dose-Response Relationship, Drug; D004357:Drug Synergism; D006736:Horses / Q000378:metabolism*; D007700:Kinetics; D000077222:Limonene; D008297:Male; D019301:Oleic Acid / Q000494:pharmacology; D009924:Organ Culture Techniques; D012869:Skin Absorption / Q000187:drug effects*; D013729:Terpenes / Q000494:pharmacology; D014508:Urea / Q000494:pharmacology
D000894:Anti-Inflammatory Agents, Non-Steroidal; D053138:Cyclohexenes; D013729:Terpenes; D004008:Diclofenac; D019301:Oleic Acid; D014508:Urea; D000077222:Limonene