A Novel Surfactant-Free O/O Paclitaxel Ointment for the Topical Treatment of Psoriasis

Abstract

Psoriasis is an autoimmune disorder disease with pink-colored plaques and excessive proliferation which is hard to be cured completely. The study focuses on the anti-psoriatic efficacy of O/O paclitaxel ointment which can promote the assembly of microtubules and lead to death of overproliferation cells of the psoriasis epidermal. A high-speed shearing method was adopted in preparing the ointment, in which propylene carbonate was used as the internal oil phase to solve paclitaxel completely. It was characterized by the appearance, particle size, rheological behavior, and in vitro release. The amount of paclitaxel retained in normal skin and psoriatic skin was 1.00 ± 0.50 versus 1.53 ± 0.48μg/g for 0.03% PTX ointment, 1.30 ± 0.39 versus 2.77 ± 0.49μg/g for 0.1% PTX ointment, and 2.22 ± 0.92 versus 6.65 ± 0.87μg/g for 0.3% PTX ointment, respectively, which implied that paclitaxel could better retain in inflamed skin than in normal skin; also the amount of drug retained in the skin was proportional to drug content. Paclitaxel ointment displayed good topical tolerance after repeated application on normal mice skin. The therapeutic efficacy of paclitaxel ointment was evaluated with an imiquimod-induced psoriatic model. A significant improvement has been shown both in the phenotypic and histopathological features of psoriatic skin treated with the ointment. There was also a significant reduction in the epidermal thickness compared to the imiquimod group. The findings confirm that the O/O PTX ointment without any surfactant appears to be a promising approach for the treatment of psoriasis.