Abstract

Abstract We measured the binding of local anesthetic tetracaine to phosphatidylinositol (PI), dipalmitoylphoshpatidylcholine (DPPC) and PI/DPPC mixed vesicles by an equilibrium dialysis method at different pH (5.5, 7.0, 8.0) at 35 °C. The results obtained for the pure phospholipid vesicles show that tetracaine binds to PI with the polyhydroxy headgroup, rather than to twitter ionic DPPC. For mixed vesicles, the higher is the ratio of the PI in mixed vesicles, the higher is the binding number. The change in pH slightly influences the binding to PI, while it strongly influences the binding to DPPC. We calculated the binding parameters which characterize the binding isotherms based on Langmuir-type and Hill equations. The binding parameters for pure PI and DPPC vesicles well reproduce the binding isotherms for PI/DPPC mixed vesicles with different mixing ratios. The results for pure PI were compared with those previously obtained for dilauroylphosphatidic acid (DLPA) in order to examine the influence of inositol in the head group of PI on the binding of tetracaine to phospholipid vesicles.

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