Microemulsion Microstructure Influences the Skin Delivery of an Hydrophilic Drug

ABSTRACT Purpose We aimed to investigate the influence of microemulsion nanoscale organization as either oil-in-water droplets, water-in-oil droplets, or bicontinuous structures on skin delivery of drugs assisted by microemulsions. Methods Three microemulsions of different microstructure, o/w, w/o,...

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Bibliographic Details
Published in:Pharmaceutical research 2011-07, Vol.28 (7), p.1683-1695
Main Authors: Naoui, Wafa, Bolzinger, Marie-Alexandrine, Fenet, Bernard, Pelletier, Jocelyne, Valour, Jean-Pierre, Kalfat, Rafik, Chevalier, Yves
Format: Article
Language:English
Subjects:
Administration, Cutaneous
Animals
Aqueous solutions
Biochemistry
Biological and medical sciences
Biomedical and Life Sciences
Biomedical Engineering and Bioengineering
Biomedicine
Caffeine - chemistry
Caffeine - pharmacokinetics
Chromatography, High Pressure Liquid
Drug Delivery Systems
Emulsions - chemistry
Emulsions - pharmacokinetics
General pharmacology
Hydrophobic and Hydrophilic Interactions
Magnetic Resonance Spectroscopy
Medical Law
Medical sciences
Microchemistry
Microemulsions
Oils - chemistry
Pharmaceutical sciences
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Pharmacology/Toxicology
Pharmacy
Research Paper
Skin - chemistry
Swine
Water - chemistry
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Summary:ABSTRACT Purpose We aimed to investigate the influence of microemulsion nanoscale organization as either oil-in-water droplets, water-in-oil droplets, or bicontinuous structures on skin delivery of drugs assisted by microemulsions. Methods Three microemulsions of different microstructure, o/w, w/o, and bicontinuous at the skin temperature (32°C), having the same oil and water contents and containing the same ingredients were selected using the Kahlweit fish phase diagrams method. The microemulsions are quaternary mixtures of the Polysorbate 21 (Tween®21) and Sorbitan monolaurate (Span®20) surfactants, isononyl isononanoate oil and water. The microemulsion nanostructure was characterized by electrical conductivity, Pulsed Field Gradient Spin-Echo NMR and Small-Angle Neutron Scattering measurements. The Franz cell method was used to monitor skin absorption of caffeine loaded in microemulsions over 24 h exposure to excised pig skin. Results Three microemulsions with the three structures were selected, keeping the same composition but the Tween®21/Span®20 ratio. The transdermal flux of caffeine was in the order aqueous solution ≈ w/o < bicontinuous < o/w microemulsion. The o/w microemulsion allows the permeation of 50% of the applied dose within 24 h. Conclusions The structure of microemulsions is of relevance for skin absorption. The water-continuous structures allow faster transport of hydrophilic drugs.
ISSN:0724-8741
1573-904X
DOI:10.1007/s11095-011-0404-y