LAUSR

&NA; In the present study, umbelliferone ‐ phospholipids complex ‐ loaded matrix film (UPLC – MF) was developed with a goal of improving transdermal permeation and anti‐inflammatory potential of umbelliferone (UMB). Umbelliferone – phospholipids complex (UPLC) was prepared using solvent evaporation method. UPLC‐MF was prepared by simple and reproducible solvent casting method. Prepared UPLC and UPLC‐MF were both physico‐chemically characterized by Fourier transforms infrared spectroscopy (FT‐IR), differential scanning calorimetry (DSC), powder x‐ray diffraction (PXRD), proton nuclear magnetic resonance spectroscopy (1H NMR), weight variation, thickness, tensile strength, folding endurance, % elongation, moisture content and uptake Functional characterization of UPLC and UPLC‐MF was carried out by solubility analysis, in vitro dissolution, diffusion, and ex vivo permeation via dialysis and biological membrane. UPLC – MF was also evaluated for in vivo anti‐inflammatory activity using carrageenan‐induced Albino rat paw model. Design‐based optimal values for formulation and process variables of UPLC were observed to be 1:1.78, 50 °C and 2 h, respectively. Physico‐chemical characterization confirmed the formation of the complex and the film. UPLC demonstrated a higher aqueous solubility (˜11‐fold), compared to pure UMB. Rate and extent of dissolution of UMB from UPLC was enhanced significantly to that of pure UMB. Compared to UMB‐MF, the diffusion and permeation rate of UMB from UPLC‐MF enhanced significantly. The UPLC – MF improved the anti‐inflammatory potential of UMB by significant enhancement of edema inhibition (%), compared to UMB‐MF. The obtained results showed that the present combined formulation system could be employed as a promising strategy for improving transdermal permeation of UMB.