Dissolving microneedle-mediated transdermal delivery of flurbiprofen axetil-loaded pH-responsive liposomes for arthritis treatment

Arthritis exerts a major impact on people's physical health and quality of life. Flurbiprofen axetil (FA), an effective non-steroidal anti-inflammatory drug for arthritis, has been limited due to its poor solubility. To boost therapeutic impact and broaden its applicability, we created FA-loaded liposomes (FA@Lipo) with an EE% of 75% via thin-film hydration sonication. Since joint injections or transdermal patches are typically used to treat arthritis, the former has poor patient compliance and the latter has limited transdermal efficacy. Therefore, considering these two aspects, we concentrated FA@Lipo and mixed it with the microneedle matrix to form FA@Lipo loaded soluble microneedles (FA@Lipo-DMNs), which could break through the skin barrier and deliver drugs effectively while reducing patient pain. In vivo pharmacodynamic experiments indicated that FA@Lipo-DMNs had similar therapeutic efficacy and less pain compared with subcutaneous injection (SC), which improved patient compliance. FA@Lipo-DMNs reduced the swelling and inflammatory factors level (TNF-α, IL-1β) of plantar and ankle joints significantly. Histological evaluation showed that FA@Lipo-DMNs could relieved arthritis effectively. All of these results all demonstrated the bright prospects of FA@Lipo-DMNs in the treatment of arthritis.