| Résumé : |
For use of topical and transdermal formulations, besides the potency of the active substance, selection of a suitable vehicle is very crucial since it can affect both drug release and skin penetration. Factors that contribute to selection are the solubility of the drug in the vehicle, release of the drug from the vehicle into the skin and enhancement of drug penetration through the stratum corneum. The main aim of this study was to analyze the influence of the lipophilicity of the vehicles systems on liberation from the multilayer membrane system and penetration into human skin of active model substances. For this purpose three actives with different physicochemical properties, dihydroavenanthramide D, salicyloyl phytosphingosine and glycyrrhizinic acid, were chosen. Model emulsions with different amounts of the oil phase (5%, 18.5% and 40%) containing Myritol PC (propylene glycol dicaprylate/dicaprate) as the lipophilic marker component were prepared. For liberation behavior of the three substances and the liphphilic component of the emulsions, the solvent drag theory could be suggested. Penetration profiles of the two model substances (dihyroave-nanthramide D and glycyrrhizinic acid) were investigated.
An increasing amount of lipid phase in emulsions did not affect the penetration profile of the substances and the lipophilic marker component in skin and the above mentioned solvent drag theory could not explain the penetration profile of the active model components. |
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Penetration studies of active model substances from an O/W emulsion - Influence of the lipophilicity of the formulation in human skin in IFSCC MAGAZINE, Vol. 15, N° 3 (07-08-09/2012)
