Phosphatidylcholine embedded micellar systems: Enhanced permeability through rat skin

Aviram Spernath, Abraham Aserin, Amnon C. Sintov, Nissim Garti

    Research output: Contribution to journalArticlepeer-review

    37 Scopus citations

    Abstract

    Micellar and microemulsion systems are excellent potential vehicles for delivery of drugs because of their high solubilization capacity and improved transmembrane bioavailability. Mixtures of propylene glycol (PG) and nonionic surfactants with sodium diclofenac (DFC) were prepared in the presence of phosphatidylcholine (PC) as transmembrane transport enhancers. Fully dilutable systems with maximum DFC solubilization capacity (SC) at pH 7 are presented. It was demonstrated that the concentrates underwent phase transitions from reverse micelles to swollen reverse micelles and, via the bicontinuous transitional mesophase, into inverted O/W microstructures. The SC decreases as a function of dilution. DFC transdermal penetration using rat skin in vitro correlated with SC, water content, effect of phospholipid content, presence of an oil phase, and ethanol. Skin penetration from the inverted bicontinuous mesophase and the skin penetration from the O/W-like microstructure were higher than that measured from the W/O-like droplets, especially when the micellar system containing the nonionic surfactant, sugar ester L-1695, and hexaglycerol laurate. PC embedded within the micelle interface significantly increased the penetration flux across the skin compared to micellar systems without the embedded PC at their interface. Moreover, the combination of PC with HECO40 improved the permeation rate (P) and shortened the lag-time (TL).

    Original languageEnglish
    Pages (from-to)421-429
    Number of pages9
    JournalJournal of Colloid and Interface Science
    Volume318
    Issue number2
    DOIs
    StatePublished - 15 Feb 2008

    Keywords

    • Diclofenac
    • Microemulsions
    • Permeability
    • Phosphatidylcholine
    • Transdermal drug delivery

    ASJC Scopus subject areas

    • Electronic, Optical and Magnetic Materials
    • Biomaterials
    • Surfaces, Coatings and Films
    • Colloid and Surface Chemistry

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