Effect of tetracaine on dynamic reorganization of lipid membranes

To understand the intrinsic influence of a drug on lipid membranes is of critical importance in pharmacological science. Herein, we report fluorescence microscopy analysis of the interaction between the local anesthetic tetracaine (TTC) and planar supported lipid bilayers (SLBs), as model membranes. Our results show that TTC increases lipid chain mobility, destabilizes the SLBs and remarkably induces membrane disruption and solubilization. Upon TTC binding, a local curvature change in the bilayer was observed, which led to the subsequent formation of up to 20-μm-long flexible lipid tubules as well as the formation of micron-size holes. Quantitative analysis revealed that membrane solubilization process can be divided into two distinct different stages as a function of TTC concentration. In the first stage (