Development and Evaluation of an Innovative S-Flurbiprofen-Diethylamine Emulgel With Superior Transdermal Delivery and Analgesic Activity

J Biomed Mater Res A. 2025 Jul;113(7):e37936. doi: 10.1002/jbm.a.37936.

Abstract

This study aimed to develop an innovative (S-flurbiprofen)-diethylamine (SFP-DEA) emulgel formulation via incorporating SFP as the active pharmaceutical ingredient within a carbomer 940 gel matrix. SFP-DEA emulgel was synthesized by dissolving SFP-DEA in the aqueous phase of an oil-in-water (O/W) emulsion, followed by dispersion into a carbomer 940 gel matrix. The physicochemical stability of SFP-DEA emulgel was evaluated via centrifuge, temperature swing test, high temperature, and long-term storage at ambient conditions. Ex vivo SFP transdermal delivery of SFP-DEA emulgel was evaluated using a Franz diffusion cell combined with excised rat skin. The in vivo analgesic activity and skin irritation test of SFP-DEA emulgel were evaluated using a mouse knee osteoarthritis model and healthy rats, respectively. Results demonstrated that SFP-DEA emulgel showed robust physicochemical stability and retain a final SFP content of 1.5% (w/w). Ex vivo transdermal study demonstrated that EMG5 (the emulgel optimized with laurocapram and menthol as penetration enhancers) achieved an 8-h cumulative SFP transdermal flux of 741.28 μg/cm2 (44.23% of the administered dose), which is 27.94-fold higher than that of Loqoa (SFP tapes). In addition, SFP-DEA emulgel demonstrated rapid analgesic efficacy, with an 84.36% pain inhibition rate within 30 min in the osteoarthritis model, and elicited no signs of skin irritation in rats. In conclusion, the SFP-DEA emulgel developed herein exhibits high stability, enhanced transdermal delivery, preliminary analgesic activity, and favorable safety profiles, positioning it as a promising topical therapeutic candidate.

Keywords: S‐flurbiprofen; analgesic activity; emulgel; skin irritation; transdermal delivery.

MeSH terms

  • Administration, Cutaneous
  • Analgesics* / administration & dosage
  • Analgesics* / pharmacology
  • Analgesics* / therapeutic use
  • Animals
  • Emulsions
  • Flurbiprofen* / administration & dosage
  • Flurbiprofen* / chemistry
  • Flurbiprofen* / pharmacokinetics
  • Flurbiprofen* / pharmacology
  • Flurbiprofen* / therapeutic use
  • Gels
  • Male
  • Mice
  • Rats
  • Rats, Sprague-Dawley
  • Skin / drug effects
  • Skin / metabolism

Substances

  • Analgesics
  • Gels
  • Flurbiprofen
  • Emulsions