Positively and negatively charged submicron emulsions for enhanced topical delivery of antifungal drugs.
Charged submicron emulsions are a priori interesting candidates for the delivery of drugs in and/or through the skin. In the present study, it was possible by using stearylamine or deoxycholic acid (DCA) to incorporate either econazole or miconazole nitrate, respectively, in positively and negatively charged submicron emulsions. The investigation of the relationship between the physicochemical properties of the vehicles, especially the charge of the emulsion and skin permeation, was conducted ex vivo during percutaneous absorption experiments using hairless female rat skin. In addition, drug quantification was carried out using two different analytical techniques (HPLC and radioactivity measurements) in order to examine if the drug analysis approach might affect the results. The results clearly indicate that the surface-modified droplets have a significant influence on the diffusion through the skin. Furthermore, the method of preparation of the formulation and subsequently the analytical method of drug concentration measurement are able to influence the results of percutaneous experiment.
Piemi
M P
MP
Laboratory of Dermopharmacology, Faculty of Pharmacy, University Paris-South, 5, Rue Jean-Baptiste Clément, 92296 Châtenay-Malabry, France.
Korner
D
D
Benita
S
S
MartyJP
D000287:Administration, Topical; D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004058:Diffusion; D004464:Econazole / Q000008:administration & dosage / Q000493:pharmacokinetics; D004563:Electrochemistry; D004655:Emulsions; D005079:Excipients; D005260:Female; D066298:In Vitro Techniques; D008825:Miconazole / Q000008:administration & dosage / Q000493:pharmacokinetics; D010316:Particle Size; D051381:Rats; D014280:Triglycerides
D000935:Antifungal Agents; D004655:Emulsions; D005079:Excipients; D014280:Triglycerides; D004464:Econazole; D008825:Miconazole