Topical emulsions containing ceramides: Effects on the skin barrier function and anti-inflammatory properties



The barrier properties of the stratum corneum (SC) are largely dependent on the intactness of the lipid lamellae that surround the corneocytes. Ceramides, fatty acids, and cholesterol together with hydrocortisone (HC) have thus been proposed as protective or therapeutic agents against xerosis and atopic dermatitis (AD). However, topical delivery of these substances is still a challenge because of the excellent barrier function of the skin. The aim of the present study was to develop a formulation with combined anti-inflammatory/barrier repair properties. In order to achieve this goal, a new non-ionic O/W emulsion (CerEmulsion) containing skin barrier lipids and HC was prepared. Its physicochemical and microbiological stability and skin permeation performance were compared to a blank emulsion (NoCerEmulsion). Placebos described as PlaceboCerEmulsion and PlaceboNoCerEmulsion of CerEmulsion and NoCerEmulsion, respectively, were also prepared in order to study the transepidermal water loss (TEWL) profiles. The emulsions presented white glossy and pourable characteristics with an acidic pH. CerEmulsion showed smaller droplet sizes and higher viscosity values (5000 mPas) while NoCerEmulsion presented viscosity values of 2000 mPas. Crystalline structures were prominent in both emulsions. The microbiological analysis showed that the results were within the established specification limits. CerEmulsion and NoCerEmulsion have shown similar release profiles and CerEmulsion presented a similar anti-inflammatory activity in vivo when compared with a commercially available 1% HC emulsion. Both emulsions were chemically, physically, and microbiologically stable. TEWL was significantly lower for the group treated with PlaceboCerEmulsion, suggesting that skin hydration was higher with this ceramide-containing formulation.

Practical applications: In this work, the authors develop and characterize a new non-ionic HC/ceramide-dominant O/W emulsion as a topical therapy for the improvement of skin barrier abnormalities in atopic dermatitis (AD). This unique formulation includes high concentrations of three lipids (ceramides, cholesterol, and free fatty acids) and paraffin. Its use is recommended for AD patients ≥6 months of age. It is also indicated for the management and relief of burning and itching associated with various dermatoses, including AD, irritant contact dermatitis, and radiation dermatitis.