Microemulsions as colloidal vehicle systems for dermal drug delivery. Part V: Microemulsions without and with glycolipid as penetration enhancer.
The aim of this study was to investigate the dermal administration of a highly hydrophilic model drug, diphenhydramine (DPH), in colloidal systems with an aqueous colloidal phase in the presence of a glycolipid (GL) as a penetration modifier. Dermal penetration of DPH, GL, and isopropylpalmitate (IPP) from ME systems without GL and with GL as well as from a hydrogel used as standard formulation were estimated in vitro using human skin. The penetration of the drug, the oil (IPP), and the GL was measured with highly sensitive HPLC, HPLC-MS, and GC-MS assays, respectively. It could be shown that penetration modifier GL is penetrating very fast, and to a high extent into and through the human skin. In contrast, the penetration of IPP used as oily phase in the ME is limited. When incorporated in the ME systems GL and DPH was accumulated in the viable epidermis and in the dermis. Using ME containing a penetration modifier such as GL, a slight additional enhancing effect could be observed, particularly concerning the penetration of DPH into the acceptor fluid when a highly hydrophilic drug such as DPH was applied.
Neubert
Reinhard H H
RH
Martin-Luther-University Halle-Wittenberg, College of Pharmacy, Institute of Pharmaceutics and Biopharmaceutics, Wolfgang-Langenbeck-Strasse 4, D-06120 Halle, Germany. neubert@pharmazie.uni-halle.de
Schmalfuss
Ulrike
U
Wolf
Raik
R
Wohlrab
Wolfgang A
WA
D000287:Administration, Topical; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D003102:Colloids / Q000737:chemistry / Q000494:pharmacology; D004155:Diphenhydramine / Q000008:administration & dosage / Q000493:pharmacokinetics; D004655:Emulsions; D008401:Gas Chromatography-Mass Spectrometry; D006017:Glycolipids / Q000737:chemistry* / Q000494:pharmacology*; D006634:Histamine H1 Antagonists / Q000008:administration & dosage / Q000493:pharmacokinetics; D006801:Humans; D020100:Hydrogels; D066298:In Vitro Techniques; D013058:Mass Spectrometry; D014677:Pharmaceutical Vehicles / Q000737:chemistry* / Q000494:pharmacology*; D012869:Skin Absorption / Q000187:drug effects*
D003102:Colloids; D004655:Emulsions; D006017:Glycolipids; D006634:Histamine H1 Antagonists; D020100:Hydrogels; D014677:Pharmaceutical Vehicles; D004155:Diphenhydramine