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-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.
Central Research Laboratory, Pias Corporation, 1-3-1 Murotani, Nishi-ku, Kobe, Japan.
Haruyoshi
H
Seino
Central Research Laboratory, Pias Corporation, 1-3-1 Murotani, Nishi-ku, Kobe, Japan.
Yukari
Y
Arai
Faculty of Life and Environmental Science, Prefectural University of Hiroshima, 562 Nanatsuka, Shobara, Japan.
Norio
N
Nagao
Central Research Laboratory, Pias Corporation, 1-3-1 Murotani, Nishi-ku, Kobe, Japan.
Noriyasu
N
Ozawa
Central Research Laboratory, Pias Corporation, 1-3-1 Murotani, Nishi-ku, Kobe, Japan.
Kazuhiko
K
Hamada
D000279:Administration, Cutaneous; D002412:Cations / Q000737:chemistry; D048271:Chitosan / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D007529:Isoflavones / Q000008:administration & dosage* / Q000737:chemistry; D008544:Melanocytes / Q000187:drug effects / Q000378:metabolism; D008823:Micelles; D010636:Phenols / Q000008:administration & dosage* / Q000737:chemistry; D011108:Polymers / Q000737:chemistry; D012867:Skin / Q000187:drug effects / Q000378:metabolism; D012869:Skin Absorption
D002412:Cations; D004337:Drug Carriers; D007529:Isoflavones; D008823:Micelles; D010636:Phenols; D011108:Polymers; D048271:Chitosan; C107601:glabridin
Am J Clin Dermatol. 2000 Sep-Oct;1(5):261-8
11702317
Biomaterials. 1989 Oct;10 (8):574-6
2605289
Br J Pharmacol. 2014 Jun;171(12):3037-50
24641665
Arch Pharm Res. 1999 Jun;22(3):232-6
10403123
Hum Pathol. 2013 Oct;44(10):2071-4
23791398
Mol Pharmacol. 2008 Dec;74(6):1576-86
18801917
J Am Acad Dermatol. 1996 Jan;34(1):29-33
8543691
Acta Biochim Pol. 2009;56(2):343-53
19543555
Acta Biomater. 2013 Jun;9(6):6790-7
23462554
J Theor Biol. 1990 Mar 8;143(1):123-38
2359315
Pigment Cell Res. 1998 Dec;11(6):355-61
9870547
Toxicol In Vitro. 2004 Jun;18(3):231-43
15046769
Arch Dermatol Res. 2015 Jan;307(1):89-98
25398276
Anticancer Res. 1998 Sep-Oct;18(5B):3709-15
9854482
Phytother Res. 2012 Aug;26(8):1107-12
22162275
Exp Dermatol. 2016 Jul;25(7):501-4
26998907
J Agric Food Chem. 2003 Feb 26;51(5):1201-7
12590456
Mol Pharm. 2006 Mar-Apr;3(2):152-60
16579644
Acta Biochim Pol. 2013;60(3):313-21
23828776
Pharm Res. 1998 Dec;15(12):1844-50
9892467
Proc Natl Acad Sci U S A. 2005 Mar 29;102(13):4688-93
15774584
Int J Pharm. 2003 Jan 16;250(2):359-69
12527163
Biomaterials. 2005 Oct;26(28):5617-23
15878366
J Pharm Pharmacol. 1994 Dec;46(12):982-5
7714722
Colloids Surf B Biointerfaces. 2007 Apr 1;55(2):192-9
17223019
Physiol Rev. 2004 Oct;84(4):1155-228
15383650
J Pharm Sci. 1987 Oct;76(10):765-73
3123641
Pigment Cell Res. 1998 Feb;11(1):12-7
9523330
PLoS One. 2012;7(12):e53314
23285276
PLoS One. 2012;7(1):e30899
22292072
Pigment Cell Melanoma Res. 2012 Jan;25(1):14-27
21834848
J Pharm Bioallied Sci. 2012 Jan;4(1):2-9
22368393
Biosci Biotechnol Biochem. 2010;74(5):918-22
20460709
J Immunol Methods. 1998 Apr 15;213(2):157-67
9692848
Biosci Biotechnol Biochem. 1995 Oct;59(10):1901-4
8534983