Preparation of lornoxicam dissolving microneedles and pharmacodynamic studies on rheumatoid arthritis
OBJECTIVE To prepare and characterize lornoxicam dissolving microneedle patches and evaluate its anti-rheumatoid arthritis efficacy.METHODS Lomoxicam dissolving microneedles(LN-DMNs)were prepared by stepwise drying method,and the drug loading was determined by HPLC.The morphology,stability,skin puncture performance and recovery per-formance of the prepared microneedles were respectively studied by scanning electron microscopy,intradermal dissolution test and puncture test.The transdermal properties were studied in vitro by the Franz diffusion cell method.Therapeutic effects of LN-DMNs on rheumatoid arthritis in rats investigated by pharmacodynamic assays.RESULTS Microneedles were neatly arranged,the shape of the needles was good,the drug content of the whole piece was(154.07±5.09)μg,the needles had good mechanical properties and could leave obvious holes in rat skin.After treatment with the microneedles,the rat skin could be restored to the original condition within 6 hours.The cumulative penetration of LN-DMNs within 36 h was(78.39±1.15)μg·cm-2,and the cumulative penetration rate was 90.06％.The results of pharmacodynamic experiments showed that LN-DMNs could signifi-cantly inhibit joint swelling in rheumatoid arthritis rats,significantly reduce the serum levels of TNF-α,IL-1β,splenic index and thymic index(P＜0.01)and suppress synovial inflammation.CONCLUSION The prepared LN-DMNs has good performance,and can promote the transdermal delivery of lonoxicam,which are promising for clinical application.
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