Synergistic permeability enhancing effect of lysophospholipids and fatty acids on lipid membranes |
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Authors: | Davidsen Jesper Mouritsen Ole G Jørgensen Kent |
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Affiliation: | Department of Pharmaceutics, The Royal Danish School of Pharmacy, Universitetsparken 2, DK-2100 Copenhagen, Denmark. |
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Abstract: | The permeability-enhancing effects of the two surfactants, 1-palmitoyl-2-lyso-sn-gycero-3-phosphocholine (lysoPPC) and palmitic acid (PA), on lipid membranes that at physiological temperatures are in the gel, fluid, and liquid-ordered phases were determined using the concentration-dependent self-quenching properties of the hydrophilic marker, calcein. Adding lysoPPC to lipid membranes in the gel-phase induced a time-dependent calcein release curve that can be described by the sum of two exponentials, whereas PA induces a considerably more complex release curve. However, when lysoPPC and PA were added simultaneously in equimolar concentrations, a dramatic synergistic permeability-enhancing effect was observed. In contrast, when both lysoPPC and PA are added to liposomal membranes that are in the fluid or liquid-ordered phases, no effect on the transmembrane permeation of calcein was observed. |
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