Topical delivery of diclofenac into and across equine skin from a novel liquid diclofenac epolamine formulation

J Vet Pharmacol Ther. 2016 Dec;39(6):578-583. doi: 10.1111/jvp.12307. Epub 2016 Mar 31.

Abstract

The aim was to investigate diclofenac delivery into and across equine skin in vitro using Franz diffusion cells from a novel diclofenac epolamine (DIC-EP; 1.3%) formulation and to compare the results to those of Surpass® (1% diclofenac sodium liposomal cream) and a 1% aqueous solution of diclofenac sodium. Skin was harvested from the lower legs of Freiberger geldings immediately after slaughter and sliced to a thickness of ~2 mm. Skin samples were divided into two groups [Group 1: 1 year old (n = 2) and Group 2: 6-8 years old (n = 3)]. Cumulative permeation of diclofenac in Groups 1 and 2 after 24 h using diclofenac sodium solution was 1.91 ± 0.27 and 1.76 ± 0.34 μg/cm2 , respectively. The values for Surpass® and DIC-EP were 3.2 ± 0.8/3.3 ± 0.7 μg/cm2 and 230 ± 59/89.2 ± 32.5 μg/cm2 , respectively. Thus, diclofenac permeation from DIC-EP was significantly greater and appeared to show an age-dependent effect. Mathematical modelling showed that the DIC-EP formulation significantly increased diclofenac partitioning into the skin and a linear correlation was observed between steady-state flux and the partition parameter. Greater skin deposition of diclofenac was also observed with DIC-EP. These preliminary results suggest that the DIC-EP formulation may be effective in treating inflammatory conditions in horses.

MeSH terms

  • Administration, Cutaneous
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics*
  • Diclofenac / administration & dosage
  • Diclofenac / analogs & derivatives*
  • Diclofenac / pharmacokinetics
  • Horses*
  • Skin / drug effects*
  • Skin Physiological Phenomena

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • diclofenac hydroxyethylpyrrolidine
  • Diclofenac