The influence of alcohol, propylene glycol and 1,2-pentanediol on the permeability of hydrophilic model drug through excised pig skin.
Alcohol and glycol including 1,2-pentanediol, a new product in this field, were examined for their transdermal penetration enhancing in vitro properties using pig skin and caffeine as a model drug. In order to investigate a possible influence of these compounds, we followed diffusion from an aqueous solution with caffeine followed by a series of different vehicles, their compositions were: (1) in water as a control; (2) in propylene glycol/ethanol/water (25:25:48; v/v/v); (3) in 1,2-pentanediol/water (2.5:95.5, v/v); (4) in 1,2-pentanediol/water (5:93, v/v); in propylene glycol/water (5:93; v/v); and in ethanol/water (5:93; v/v). The stratum corneum/vehicle partition coefficients (K(m)), maximum flux (J), enhancement factor (EF), 24-h receptor concentration (Q(24h)) were determined and compared to control values (caffeine in water). Permeation was also expressed in percentage of the applied dose absorbed in the different compartments. In all test models, caffeine was released and penetrated into pig skin. The 1,2-pentanediol was presented as the most effective enhancer; with a low proportion of this compound (only 5%), caffeine penetrated the skin quicker and in a greater extent. While this compound showed promise as penetration enhancer, further study was required to determine its effectiveness with others drugs and its irritation potential.
Duracher
Lucie
L
IBMM UMR 5247 CNRS-UM1-UM2, Faculté de Pharmacie, Université de Montpellier I, Montpellier Cedex 5, France. lucie.duracher@etu.univ-montp1.fr
Blasco
Laurent
L
Hubaud
Jean-Claude
JC
Vian
Laurence
L
Marti-Mestres
Gilberte
G
D000279:Administration, Cutaneous; D000818:Animals; D002110:Caffeine / Q000008:administration & dosage / Q000493:pharmacokinetics*; D002626:Chemistry, Pharmaceutical; D000431:Ethanol / Q000737:chemistry; D005079:Excipients / Q000737:chemistry*; D006018:Glycols / Q000737:chemistry*; D066298:In Vitro Techniques; D010420:Pentanes; D010539:Permeability; D014677:Pharmaceutical Vehicles / Q000737:chemistry; D019946:Propylene Glycol / Q000737:chemistry; D012869:Skin Absorption; D013552:Swine; D014867:Water / Q000737:chemistry
D005079:Excipients; D006018:Glycols; D010420:Pentanes; D014677:Pharmaceutical Vehicles; D014867:Water; D002110:Caffeine; D000431:Ethanol; C452500:1,2-pentanediol; D019946:Propylene Glycol