Binary Ethosomal Gel for Enhanced Transdermal Delivery of Tazarotene: Development, Refinement, in vitro Evaluation, and Skin Penetration Investigations

Abstract

Background: Tazarotene (TZ) is a novel acetylenic class retinoid that selectively targets RARβ/γ. It is not particularly soluble or bioavailable, yet it is used to treat melanoma. Objective: To improve the tazarotene gel formula's transdermal distribution. Methods: TZ-incorporated binary ethosomes (TZ-BES) were developed for the current study. The cold technique and optimized Box-Behnken statistical design tools were used to synthesize the TZ-BES. The improved ethosome (TZ-BES13) was mixed with carbopol gel and tested for stability and ex vivo skin penetration, as well as viscosity, pH, spreadability, and drug content. Results: The optimal ethosomes (TZ-BES13) had a vesicle size of 168 nm, a PDI of 0.367, a zeta potential of -30 mV, and an entrapment effectiveness of 79.94%. TZ is enclosed in the ethosome matrix, as seen by the differential scanning calorimetry thermogram. FTIR shows that the TZ and additives are compatible. TZ-BES13-G2, the optimized TZ-BES13 gel, has a spreadability of 7.82 cm2, a pH of 6.52, a viscosity of 17235, and a drug content of 99.82±1.04%. Compared to the plan TZ-gel (43.54%), the TZ-BES13-G2 exhibits a much higher TZ release (89.22%). In 6 hours, rat abdomen skin permeability for TZ-BES13-G2 was 66.22±3.31%, much greater than that of plan TZ-gel (24.67%). The flow of TZ-BES13-G2 was 2.68 times greater than that of plan TZ-gel. The stability analysis showed that the formulation's properties had not changed significantly. Conclusion: Ethosomal gel offers an alternative mode of TZ administration when used topically.