Abstract
Partially myristoylated chitosan pyrrolidone carboxylate (PMCP) is a cationic amphiphilic chitosan derivative. Glabridin (Glab) from licorice root extracts is a hydrophobic antimelanogenic agent. Here we assessed the effects of cationic Glab-containing polymeric micelles derived from PMCP (Glab/PMCP-PM) on the ability of Glab to penetrate the skin and inhibit melanogenesis using a human skin model. The amount of Glab absorbed 24 h after the application of Glab/PMCP-PM was approximately four times higher than that of conventional oil-in-water micelles (control) prepared using Tween 60. Further, the release of IL-1α, a mediator of inflammation, was not detected. Treatment with Glab/PMCP-PM significantly increased the inhibition of melanogenesis compared with control. The inhibition of melanogenesis depends upon the enhanced ability of Glab to penetrate the skin, particularly the epidermis. Moreover, the inhibition of melanogenesis and the cationic potential of the Glab/PMCP-PM levels were increased by the cationic phospholipid copolymer. Therefore, Glab/PMCP-PM shows potential as an effective transdermal delivery system for treating skin hyperpigmentation.
Highlights
Skin hyperpigmentation is caused by the overproduction of melanins, which are synthesized by tyrosinase and melanogenesis related proteins (MRP) [1]
We previously reported that Partially myristoylated chitosan pyrrolidone carboxylate (PMCP) is a cationic amphiphilic chitosan derivative [21]
Because the human skin is negatively charged at a physiological pH and is cation permselective [22], this study suggests that Glab/PMCP-PM, which forms cationic polymer micelles having an interface rich in charged amino groups, enhances the percutaneous delivery of Glab to the human skin model
Summary
Skin hyperpigmentation is caused by the overproduction of melanins, which are synthesized by tyrosinase and melanogenesis related proteins (MRP) [1]. Tyrosinase mediates melanogenesis, which frequently occurs in damaged human skin. It has reported that L-tyrosine and L-DOPA enhance tyrosinase and its transport into melanosomes results in an increase in melanin pigmentation [2,3]. Of facial skin, is often masked using make-up cosmetics. The treatment of injured skin is invariably an ongoing process that requires considerable effort [4]. There is great demand for medicated skin care cosmetics and medications for external application that are clinically designed to remedy or prevent skin disorders
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