Development of microemulsions of suitable viscosity for cyclosporine skin delivery

Publication date: 10 July 2018 Source:International Journal of Pharmaceutics, Volume 545, Issues 1–2 Author(s): Marta Benigni, Silvia Pescina, Maria Aurora Grimaudo, Cristina Padula, Patrizia Santi, Sara Nicoli Psoriasis is a widespread chronic disease affecting 2–4% of the population in Western countries. Its mild-to-moderate form, representing approximately 80% of the total cases, is treated by topical application, with corticosteroid being the standard treatment. However, in case of psoriasis, no single treatment works for every patient and optimizing topical therapy is a key aspect. A possible alternative is represented by cyclosporine, an immunosuppressant cyclic peptide administered orally in the treatment of the severe form. Its topical application could avoid the problems related to systemic immunosuppression, but the unfavourable physico-chemical properties (MW: 1202 Da; LogP ≈ 3) hinder its permeation across the stratum corneum. The aim of the paper was the preparation, characterization and ex-vivo evaluation of cyclosporine loaded microemulsions using oleic acid as oil phase, either Tween®80 or a soluble derivative of vitamin E (TPGS) as surfactants and either Transcutol®, propylene glycol or 1,3 propanediol as co-surfactants. The issue of formulation viscosity was also addressed 1) by evaluating the thickening of Tween®80-based microemulsions by direct addition of different rheological modifiers, 2) by building pseudo-ternary phase diagrams ...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research