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

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...

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Bibliographic Details
Published in:PloS one 2016-10, Vol.11 (10), p.e0164061-e0164061
Main Authors: Seino, Haruyoshi, Arai, Yukari, Nagao, Norio, Ozawa, Noriyasu, Hamada, Kazuhiko
Format: Article
Language:English
Subjects:
Administration, Cutaneous
Analysis
Biology and Life Sciences
Cationic polymerization
Cations - chemistry
Chitosan
Chitosan - chemistry
Copolymers
Cosmetics
Drug Carriers - chemistry
Drug delivery
Epidermis
Glycyrrhiza glabra
Homogenization
Humans
Hydrophobic and Hydrophilic Interactions
Hydrophobicity
Hyperpigmentation
Inhibition
Isoflavones - administration & dosage
Isoflavones - chemistry
Laboratories
Medicine and Health Sciences
Melanocytes - drug effects
Melanocytes - metabolism
Micelles
Molecular weight
Permeability
Phenols - administration & dosage
Phenols - chemistry
Phospholipids
Physical Sciences
Polymers
Polymers - chemistry
Skin
Skin - drug effects
Skin - metabolism
Skin Absorption
Surfactants
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Summary: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.
ISSN:1932-6203
1932-6203
DOI:10.1371/journal.pone.0164061