Efficient Percutaneous Delivery of the Antimelanogenic Agent Glabridin Using Cationic Amphiphilic Chitosan Micelles

PLoS One. 2016 Oct 3;11(10):e0164061. doi: 10.1371/journal.pone.0164061. eCollection 2016.

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.

MeSH terms

  • Administration, Cutaneous
  • Cations* / chemistry
  • Chitosan* / chemistry
  • Drug Carriers* / chemistry
  • Humans
  • Hydrophobic and Hydrophilic Interactions
  • Isoflavones / administration & dosage*
  • Isoflavones / chemistry
  • Melanocytes / drug effects
  • Melanocytes / metabolism
  • Micelles*
  • Phenols / administration & dosage*
  • Phenols / chemistry
  • Polymers / chemistry
  • Skin / drug effects
  • Skin / metabolism
  • Skin Absorption

Substances

  • Cations
  • Drug Carriers
  • Isoflavones
  • Micelles
  • Phenols
  • Polymers
  • Chitosan
  • glabridin

Grants and funding

The funder (Pias Corporation) provided support in the form of salaries for authors Haruyoshi Seino, but did not have any additional role in the study design, data collection and analysis, decision to publish, or preparation of the manuscript. Norio Nagao conducted joint research to instruct about this study. The specific roles of these authors are articulated in the ‘author contributions’ section.