Chemical enhancers for the absorption of substances through the skin: Laurocapram and its derivatives.
Absorption enhancers are substances used for temporarily increasing a membrane's permeability (e.g., the skin and mucosa), either by interacting with its components (lipids or proteins) or by increasing the membrane/vehicle partition coefficient. This article presents the results of biophysical and permeability studies performed with Laurocapram and its analogues. As shown, Laurocapram and its analogues present different enhancing efficacies, for most of both hydrophilic and lipophilic substances. The enhancing effect of Laurocapram (Azone) is attributed to different mechanisms, such as insertion of its dodecyl group into the intercellular lipidic bilayer, increase of the motion of the alkylic chains of lipids, and fluidization of the hydrophobic regions of the lamellate structure. Toxicological studies reveal a low toxicity for Laurocapram, and for some derivatives, a relationship exists between toxicity and the number of carbons in the alkylic chain. Very important, when applied to human skin, Laurocapram shows a minimal absorption, being quickly eliminated from circulation. However, although Laurocapram and its derivatives have been shown to provide enhancement, they have not been widely accepted because of their suspected pharmacological activity or questions about their safety.
López-Cervantes
Miriam
M
División de Estudios de Posgrado (Tecnología Farmacéutica), Facultad de Estudios Superiores Cuautitlán, Universidad Nacional Autónoma de México, Cuautitlán Izcalli, Edo. de México.
Márquez-Mejía
Eréndira
E
Cázares-Delgadillo
Jennyfer
J
Quintanar-Guerrero
David
D
Ganem-Quintanar
Adriana
A
Angeles-Anguiano
Enrique
E
D000818:Animals; D001381:Azepines / Q000009:adverse effects / Q000032:analysis* / Q000493:pharmacokinetics*; D002626:Chemistry, Pharmaceutical; D006801:Humans; D066298:In Vitro Techniques; D012869:Skin Absorption / Q000187:drug effects*; D013329:Structure-Activity Relationship
D001381:Azepines; C035229:laurocapram