preparation and evaluation of imatinib loaded transfersomal gel for the treatment of rheumatoid arthritis

in the present study, imatinib-loaded transfersomal gel (imatinib-tfs-gel) was developed to minimize the oral dosing frequency and side effects during rheumatoid arthritis (ra) therapy. imatinib-loaded transfersomes (imatinib-tfs) were prepared by the film-hydration method. the effects of lecithin content, lecithin/ ea ratio, and the type of ea on the characteristics of the imatinib-tfs were studied using a d-optimal design. morphology of imatinib-tfs was investigated using scanning electron microscopy. the optimized imatinib-tfs formulation was used to prepare imatinib-tfs-gel with the aid of carbopol 940 as the gelling agent. the optimized imatinib-tfs had a spherical shape with the particle size of 140.53 ± 0.87 nm, polydispersity index of 0.44 ± 0.01, the zeta potential of -17.63 ± 0.65 mv, encapsulation efficiency of 98.70 ± 0.38%, and release efficiency of 81.26 ± 0.70 %. ex-vivo skin permeation studies through the rat skin showed that the cumulative amount of imatinib permeated from imatinib-tfs-gel was significantly higher than that from imatinib-gel. the ra rat model indicated a substantial reduction in paw edema during the 14 days study following the application of imatinib-tfs-gel as compared with imatinib-gel. therefore, imatinib-tfs-gel can be considered as a promising drug delivery system for the treatment of ra.