Analgesic effect of S (+)-flurbiprofen plaster in a rat model of knee arthritis: analysis of gait and synovial fluid prostaglandin E2 levels

J Pharm Pharmacol. 2018 Jul;70(7):929-936. doi: 10.1111/jphp.12914. Epub 2018 Apr 1.

Abstract

Objectives: We developed S (+)-flurbiprofen plaster (SFPP), a novel NSAID patch containing S (+)-flurbiprofen (SFP), a potent cyclooxygenase (COX) inhibitor. The purpose of this study was to assess efficacy of SFPP by analysing its effect on the gait disturbance and measuring the prostaglandin E2 (PGE2 ) production in synovial fluid in a rat model of knee arthritis.

Methods: Knee inflammation was induced in rats by intra-articular injection of a yeast suspension. Subsequently, an NSAID patch containing SFP, ketoprofen or loxoprofen was applied over the affected knee. Gait was assessed at 2, 4 and 6 h after application of the patch. The PGE2 concentration in the synovial fluid was measured after the gait assessment.

Key findings: Application of SFPP (0.125, 0.25, 0.5 or 1 mg/sheet) was followed by a decrease in the visual gait score at all the doses examined. In the case of the other two NSAID patches, only the ketoprofen patch (1 or 2 mg/sheet) and loxoprofen patch (5 mg/sheet) produced a decrease in the visual gait score. All of the NSAID patches decreased the PGE2 production in the synovial fluid.

Conclusions: These results suggest the potential usefulness of SFPP as an analgesic patch in patients with inflammatory joint pain.

Keywords: NSAID patch; S (+)-flurbiprofen plaster; arthritis; gait.

MeSH terms

  • Analgesics / therapeutic use*
  • Animals
  • Arthritis, Experimental / chemically induced
  • Arthritis, Experimental / drug therapy*
  • Dinoprostone / metabolism*
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Flurbiprofen / therapeutic use*
  • Gait / drug effects*
  • Ketoprofen / therapeutic use
  • Male
  • Phenylpropionates / therapeutic use
  • Rats
  • Synovial Fluid / drug effects*
  • Synovial Fluid / metabolism*
  • Transdermal Patch

Substances

  • Analgesics
  • Phenylpropionates
  • loxoprofen
  • Flurbiprofen
  • Ketoprofen
  • Dinoprostone