Improvement of Hydration and Epidermal Barrier Function in Human Skin by a Novel Compound Isosorbide Dicaprylate

Abstract

Objective

The study involved the synthesis of a novel derivative of caprylic acid - isosorbide dicaprylate (IDC) - and the evaluation of its potential in improving water homeostasis and epidermal barrier function in human skin.

Methods

The effect of IDC on gene expression was assayed in skin organotypic cultures by DNA microarrays. The results were then confirmed for a few key genes by quantitative PCR, immuno- and cytochemistry. Final validation of skin hydration properties was obtained by four separate clinical studies. Level of hydration was measured by corneometer either by using 2% IDC lotion alone vs placebo or in combination with 2% glycerol lotion vs 2% glycerol only. A direct comparison in skin hydration between 2% IDC and 2% Glycerol lotions was also carried out. The epidermal barrier function improvement was assessed by determining changes in trans-epidermal water loss (TEWL) on the arms before and after treatment with 2% IDC lotion versus placebo.

Results

IDC was found to up-regulate the expression of AQP3, CD44 and proteins involved in keratinocyte differentiation as well as the formation and function of stratum corneum. A direct comparison between 2% IDC versus 2% glycerol lotions revealed a 3-fold advantage of IDC in providing skin hydration. Severely dry skin treated with 2% IDC in combination with 2% glycerol showed 133% improvement whereas 35% improvement was observed with moderately dry human skin.

Conclusion

Topical isosorbide dicaprylate favorably modulates genes involved in the maintenance of skin structure and function, resulting in superior clinical outcomes. By improving skin hydration and epidermal permeability barrier it offers therapeutic applications in skin aging.

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