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.
S Del Río-Sancho  1 ,  D Concas  2 ,  P Oreste  3 ,  G Zoppetti  3 ,  P H Briggs  4 ,  Y N Kalia  5
Affiliations
  • 1. School of Pharmaceutical Sciences, University of Geneva and University of Lausanne, Geneva, Switzerland.
  • 2. Wezen Bio AG, Fondation pour Recherches Médicales, Geneva, Switzerland.
  • 3. Glycores 2000 Srl, Milan, Italy.
  • 4. Alkhalediah Equine Hospital, Riyadh, Kingdom of Saudi Arabia.
  • 5. School of Pharmaceutical Sciences, University of Geneva and University of Lausanne, Geneva, Switzerland. [email protected].
PMID: 27030162 DOI: 10.1111/jvp.12307
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.

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