Permeability and retention studies of (-)epicatechin gel formulations in human cadaver skin.
(-)Epicatechin (EC) is a major antioxidant component of grape seed extract which has become increasingly popular in topical skin preparations. This study assessed the following: (1) the permeability through cellulose membranes of EC in three different gel formulations (Carbopol 940, Klucel, and Ultrez 10); (2) the effect of three different antioxidants (butylated hydroxytoluene (BHT), alpha-tocopherol (VE), and ascorbic acid (AA)) on the stability and penetration properties of EC; and (3) the permeability and retention of EC in Ultrez 10 gels, supplemented with BHT or VE, on human cadaver skin. Permeability studies through cellulose membranes showed that different gelling agents do not significantly affect the permeability of EC (n = 7/gel; p > 0.05). BHT and VE have antioxidant properties superior to AA (p < 0.05) and preserve 100% of the initial content of EC for 28 days. Permeation studies on cadaver human skin, following application of two anhydrous gel formulations (0.5% EC in Ultrez 10 containing BHT or VE), showed that EC was not detectable in the receiving solution. However, the EC amount in viable skin increased with time, indicating that EC penetrated and was retained in the upper part of the skin for approximately 1% and 3% of the dose for the formulations containing BHT and VE, respectively.
Suppasrivasuseth
J
J
Division of Pharmaceutical Sciences, Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, NY 11201, USA.
Bellantone
R A
RA
Plakogiannis
F M
FM
Stagni
G
G
D000180:Acrylic Resins / Q000737:chemistry*; D000975:Antioxidants / Q000737:chemistry* / Q000493:pharmacokinetics*; D001205:Ascorbic Acid / Q000737:chemistry; D002084:Butylated Hydroxytoluene / Q000737:chemistry; D002102:Cadaver; D002392:Catechin / Q000493:pharmacokinetics*; D002482:Cellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D002851:Chromatography, High Pressure Liquid; D004355:Drug Stability; D005782:Gels; D006801:Humans; D066298:In Vitro Techniques; D008567:Membranes, Artificial; D010539:Permeability; D012869:Skin Absorption / Q000187:drug effects*; D013678:Technology, Pharmaceutical; D024502:alpha-Tocopherol / Q000737:chemistry
D000180:Acrylic Resins; D000975:Antioxidants; D005782:Gels; D008567:Membranes, Artificial; C479038:carbomer; D002084:Butylated Hydroxytoluene; C006903:carbopol 940; D002392:Catechin; D002482:Cellulose; C008079:hydroxypropylcellulose; D024502:alpha-Tocopherol; D001205:Ascorbic Acid