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Microemulsion Microstructure Influences the Skin Delivery of an Hydrophilic Drug

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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.

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ACKNOWLEDGMENTS

This work was supported by a grant PHC Utique n°08G1106 for French-Tunisian cooperation.

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Authors and Affiliations

  1. Université de Lyon Laboratoire d’Automatique et de Génie des Procédés (LAGEP) UMR CNRS 5007, Institut des Sciences Pharmaceutiques et Biologiques Laboratoire de Dermopharmacie et Cosmétologie, Université Lyon 1, Villeurbanne, France

    Wafa Naoui, Marie-Alexandrine Bolzinger, Jocelyne Pelletier, Jean-Pierre Valour & Yves Chevalier

  2. Institut National de Recherche et d’Analyse Physico-chimique, 2020, Sidi Thabet, Tunisia

    Wafa Naoui & Rafik Kalfat

  3. Université de Lyon, Centre Commun de RMN, Université Lyon 1, Villeurbanne, France

    Bernard Fenet

  4. Laboratoire de Dermopharmacie et Cosmétologie, Institut des Sciences Pharmaceutiques et Biologiques, 8 av Rockefeller, 69373, Lyon cedex 08, France

    Marie-Alexandrine Bolzinger

  5. LAGEP, Université Lyon 1, 43 bd 11 Novembre, 69622, Villeurbanne cedex, France

    Marie-Alexandrine Bolzinger

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  1. Wafa Naoui
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  2. Marie-Alexandrine Bolzinger
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  3. Bernard Fenet
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Correspondence to Marie-Alexandrine Bolzinger.

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Naoui, W., Bolzinger, MA., Fenet, B. et al. Microemulsion Microstructure Influences the Skin Delivery of an Hydrophilic Drug. Pharm Res 28, 1683–1695 (2011). https://doi.org/10.1007/s11095-011-0404-y

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  • DOI: https://doi.org/10.1007/s11095-011-0404-y

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