Simultaneous determination of active component and vehicle penetration from F-DPPC liposomes into porcine skin layers.
Liposomes have been used as innovative delivery vehicles on skin for a number of years due to their positive influence on skin penetration. However, until now it is not entirely clear how and by which mechanism enhancement is achieved. In the present study, the skin permeation of a model substance incorporated into liposomes and a control formulation was compared to study the influence of the vehicle in Franz-type diffusion cell experiments. Furthermore, the penetration depths of both components were studied by simultaneous determination of the active substance and the vehicle component during tape stripping studies and horizontal sectioning. For these purposes we prepared liposomes with 1-palmitoyl-2-(16-fluoropalmitoyl)-sn-glycero-3-phosphocholine (F-DPPC), the monofluorinated analogue of dipalmitoylphosphaditylcholine (DPPC) loaded with sodium fluorescein (SoFl). A sodium-fluorescein solution was used as control formulation. While the semi-solid F-DPPC liposomes and the SoFl-solution performed equally well with similar permeation profiles during skin diffusion experiments, superior penetrated amounts of SoFl into the stratum corneum (SC) from F-DPPC liposomes compared to the SoFl-solution were observed possibly due to a "push" exerted by the vehicle F-DPPC. We also showed that SoFl penetrated through SC into the viable epidermis.
Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Life Sciences, University of Vienna, Vienna 1090, Austria.
Denise-Silvia
DS
Mahrhauser
Department of Pharmacognosy, University of Vienna, Vienna 1090, Austria.
Gottfried
G
Reznicek
Department of Pharmaceutical Chemistry, Faculty of Life Sciences, University of Vienna, Vienna 1090, Austria.
Sebastian
S
Gehrig
Department of Pharmaceutical Chemistry, Faculty of Life Sciences, University of Vienna, Vienna 1090, Austria.
Antonia
A
Geyer
Department of Pharmaceutical Chemistry, Faculty of Life Sciences, University of Vienna, Vienna 1090, Austria.
Manfred
M
Ogris
Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Life Sciences, University of Vienna, Vienna 1090, Austria.
Ruth
R
Kieweler
Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Life Sciences, University of Vienna, Vienna 1090, Austria; Research Platform "Characterisation of Drug Delivery Systems on Skin and Investigations of Involved Mechanisms", University of Vienna, Vienna 1090, Austria. Electronic address: claudia.valenta@univie.ac.at.
Claudia
C
Valenta
D000818:Animals; D016503:Drug Delivery Systems; D004817:Epidermis / Q000378:metabolism; D005079:Excipients / Q000737:chemistry*; D019793:Fluorescein / Q000008:administration & dosage* / Q000493:pharmacokinetics; D008081:Liposomes; D010713:Phosphatidylcholines / Q000737:chemistry*; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption; D013552:Swine; D014018:Tissue Distribution
C115319:1-palmitoyl-2-(16-fluoropalmitoyl)phosphatidylcholine; D005079:Excipients; D008081:Liposomes; D010713:Phosphatidylcholines; D019793:Fluorescein
F-DPPC; Fluorescein sodium salt; Mass spectrometry; Penetration depth; Porcine skin layers; Vehicle skin penetration