Baicalin loaded transethosomes for rheumatoid arthritis: Development, characterization, pharmacokinetic and pharmacodynamic evaluation

Abstract

The present research study limns the preparation of Baicalin-loaded transethosomes (BCL-TE) to improve BCL solubility, bioavailability and permeation through skin layers for transdermal delivery. BCL-TE was formulated using thin-film hydration method and optimization was done using Box-Behnken design (BBD). BCL-TEopt was characterized for Polydispersity index (PDI), vesicle size, entrapment efficiency, zeta potential and in vitro BCL release. For further evaluation, Pharmacokinetic study, Transmission electron microscopy (TEM), Skin permeation study and Confocal scanning laser microscopy (CLSM) were performed withal. The BCL-TEopt presented spherical and sealed shape vesicles with small vesicle size of 141.2 nm, entrapment efficiency of 76.39%, PDI of 0.1135 and in vitro release of 65.32%. The CLSM study unveiled that the developed formulation has greater permeation of BCL across the skin layers in comparison with the BCL suspension gel. The pharmacokinetic study demonstrated Cmax and AUC0–24 h of 7.94 ± 0.51 μg/ml and 42.92 ± 7.90 μg. h/ml via transdermal route in comparison to Cmax and AUC0–24 h of 3.94 ± 1.91 μg/ml and 24.96 ± 9.76 μg. h/ml presented by BCL-TE oral administration. The in vivo study revealed that the BCL-TE gel has good anti-arthritic potential in comparison with the standard diclofenac gel which was evinced by radiographic analysis and histopathological studies. Further, skin irritation study on Wistar albino rats confirm that the developed BCL-TE formulation is safer for skin application. The current investigation corroborated that the prepared TE vesicle formulation is a treasured carrier for the BCL transdermal delivery for the management of rheumatoid arthritis.