Ceramide liposomes for skin barrier recovery: A novel formulation based on natural skin lipids

[Display omitted] •Stable ceramide liposomes based solely on natural skin lipids were successfully prepared.•The main stabilizing agents were cholesterol, stearic acid and urea.•Phospholipids were found to be redundant in the formulation.•The final liposomal formulation was able to efficiently resto...

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Veröffentlicht in:International journal of pharmaceutics 2021-03, Vol.596, p.120264-120264, Article 120264
Hauptverfasser: Vovesná, Aneta, Zhigunov, Alexander, Balouch, Martin, Zbytovská, Jarmila
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Sprache:eng
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Zusammenfassung:[Display omitted] •Stable ceramide liposomes based solely on natural skin lipids were successfully prepared.•The main stabilizing agents were cholesterol, stearic acid and urea.•Phospholipids were found to be redundant in the formulation.•The final liposomal formulation was able to efficiently restore the disrupted skin barrier in vitro. Diseases related to a disrupted skin barrier are accompanied by lower levels of ceramides in the stratum corneum (SC) lipid matrix. Delivering ceramides directly into damaged skin is a viable alternative to conventional corticosteroids, but is hindered by their low skin bioavailability and limited nanoformulation ability. Here, we developed stable liposomal systems containing ceramides and other SC lipids, and tested their effectiveness in skin barrier repair. Lipid film hydration and high-pressure homogenization were used to prepare different types of liposomes. To determine the stability, the particle size and polydispersity index were measured. The optimal systems were found to include ceramide 3 and 6, cholesterol and stearic acid, with 10% urea in phosphate-buffered saline as the aqueous phase. The ability of the system to repair chemically-damaged porcine skin was tested. While treatment by a standard lipid suspension reduced the passage of a model permeant only to a limited extent, drug flux through the liposomally-treated skin was much closer to permeation through intact skin. The non-homogenized liposomes were more effective than their homogenized version. These findings were also confirmed by FTIR measurements. This suggests that our approach to liposomal development has considerable potential for the repair of a disrupted skin barrier.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2021.120264