New topical microemulsions of etofenamate as sufficient management of osteoarthritis

Abstract In this study, microemulsions containing etofenamate were prepared and evaluated as dermal delivery carriers. The developed microemulsions consist of oleic acid, Span 80, Tween 20, Cremophor EL, Transcutol and ethanol. The percentage of etofenamate loading in the microemulsions was 5% (w/w). The characterization of formulations included droplet size, zeta potential, pH, conductivity, PDI, refractive index and viscosity. Moreover, ex vivo penetration study was carried out using mice abdominal skin. The developed formulations were analyzed for their cytotoxicity via MTT assay and tested for their anti-inflammatory properties opposed to LPS-stimulated nitrite prοduction in RAW 264.7 cells. As ideal formulation, M2ETF, was chosen due to its greater permeation, lower penetration as well as higher anti-inflammatory activity compared to other microemulsions.

摘要 本研究制备并评价了含依托芬那酯（etofenamate）的微乳液，将其作为皮肤递送载体。所开发的微乳液由油酸、司盘80（Span 80）、吐温20（Tween 20）、Cremophor EL、Transcutol及乙醇复配而成。微乳液中依托芬那酯的载药量为5%（质量分数，w/w）。对该系列制剂的表征指标包括粒径、ζ电位、pH值、电导率、多分散性指数（PDI）、折射率与黏度。此外，采用小鼠腹部皮肤开展离体透皮渗透实验。通过MTT法分析所开发制剂的细胞毒性，并通过检测脂多糖（LPS）刺激RAW 264.7细胞的亚硝酸盐生成水平，评价其抗炎活性。相较于其他微乳液，制剂M2ETF因具备更优异的透皮渗透性能、更低的渗透深度以及更高的抗炎活性，被选为最优制剂。