Evaluation of Topical Lifitegrast Formulations for Treatment of Psoriasis

Abstract

Background: Lifitegrast, a lymphocyte function-associated antigen-1 antagonist, was found to be useful in the treatment of psoriasis.Objectives: The study aimed to evaluate semisolid formulations of lifitegrast for their physicochemical and efficacy performance.Materials and Methods: Emulgel and ointment formulations were prepared with permissible excipients that help in increasing permeability and retention in the skin. The rheological characteristics, release rate, in vitro permeation, and biological activity in the imiquimod-induced psoriasis model in C57 mice were studied for these formulations.Results: The formulations (emulgel and ointment) were found to be homogeneous and stable, with characteristic shearthinning and viscoelastic behavior suitable for topical use. The gel formulation had the highest mean release rate, while in vitro permeation studies showed that the emulgel had superior drug permeation and retention. These formulations of lifitegrast topically (3%, 5%, and 7%) were applied twice a day on the psoriatic skin of C57 mice for 6 days, and Psoriasis Area and Severity Index scores were measured. The formulations reduced psoriatic inflammation, and the emulgel formulations were found to be significantly more efficacious than the ointment formulations.Conclusion: Lifitegrast formulations showed substantial improvement in psoriasis, owing to the optimum permeation and retention in psoriatic skin.

Keywords: Lifitegrast; gel; ointment; psoriasis; skin retention