Effect of different penetration enhancers on diclofenac permeation across horse skin

• Published in: The veterinary journal (1997) Vol. 186; no. 3; pp. 312 - 315
• Main Authors: Ferrante, M., Andreeta, A., Landoni, M.F.
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01.12.2010
• Subjects: absorption; Administration, Cutaneous; Animals; Anti-Inflammatory Agents, Non-Steroidal - administration & dosage; Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics; Cyclohexenes - pharmacology; d-Limonene; Diclofenac - administration & dosage; Diclofenac - pharmacokinetics; Diclofenac diethylamine; Dose-Response Relationship, Drug; Drug Synergism; Horse skin; horses; Horses - metabolism; in vitro studies; Kinetics; Male; Oleic acid; Oleic Acid - pharmacology; Organ Culture Techniques; Penetration enhancers; skin; Skin Absorption - drug effects; Terpenes - pharmacology; transdermal application; Urea; Urea - pharmacology; veterinary drugs; Horse skin; Urea; d-Limonene; Diclofenac diethylamine; Oleic acid; Penetration enhancers
• ISSN: 1090-0233; 1532-2971
• DOI: 10.1016/j.tvjl.2009.09.010

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.