Wednesday, 27 June 2007 - 10:20 AM
Clayton 101B
333

Structure of “flexible” liposome formulations as probed by SANS

Oluwatosin A. Ogunsola1, Margaret E.K. Kraeling2, Matthew B. Dowling1, Robert L. Bronaugh2, and Srinivasa R. Raghavan1. (1) University of Maryland, College Park, MD, (2) Food and Drug Administration, College Park, MD

Recently, there has been much interest in creating liposomes that can penetrate skin and thereby deliver their encapsulated contents for therapeutic (e.g., a drug or vaccine) or cosmetic purposes. Several studies have shown that so-called “flexible” liposomes or transfersomesTM are indeed capable of penetrating skin. These liposomes are created by mixing lipids with small amounts of a denaturing agent such as Tween 80 or an alcohol. The flexibility of these liposomes has been quantified by permeability measurements, while their skin penetration has been evaluated by confocal microscopy. In this study, we use small-angle neutron scattering (SANS) to further probe the structure in formulations that are supposed to consist of flexible liposomes. Our studies suggest that the above solutions may actually contain a combination of liposomes and micelles. In other words, the effect of adding detergent is not just to make the liposomes flexible, but also to micellize a fraction of the lipids. To our knowledge, this aspect has not been highlighted in the literature thus far. Our findings suggest a different hypothesis for the skin-penetrating action of these liposome formulations. We test this hypothesis further by examining the penetrating ability of new liposome-micelle mixtures into hairless guinea pig skin using confocal microscopy.