Abstract

Interactions between phospholipid membranes and selected drugs affecting the central nervous system (CNS) were investigated. Small, unilamellar liposomes were used as biomimetic cell membrane models. Microelectrophoretic experiments on two-component liposomes were performed using the electrophoretic light scattering technique (ELS). The effect of both positively (perphenazine, PF) and negatively (barbituric acid, BA) charged drugs on zwitterionic L-α-phosphatidylcholine (PC) membranes were analyzed. Experimental membrane surface charge density (δ) data were determined as a function of pH. Quantitative descriptions of the adsorption equilibria formed due to the binding of solution ions to analyzed two-component membranes are presented. Binding constants of the solution ions with perphenazine and barbituric acid-modified membranes were determined. The results of our research show that both charged drugs change surface charge density values of phosphatidylcholine membranes. It can be concluded that perphenazine and barbituric acid are located near the membrane surface, interacting electrostatically with phosphatidylcholine polar heads.

Highlights

  • Up-and-coming model membrane systems which mimic the fundamental structural and functional properties of natural membranes are liposomes, those formed from phosphatidylcholine—one of the predominant lipids in the cellular membrane [3,4]

  • We focused on the effect of cationic and anionic drug molecules on surface effect of cationic and anionic drug molecules on surface charge densities of zwitterionic phosphatidylcholine liposomes

  • Hydroxide, sodium, and chloride ions adsorb at the PC/PF and PC/Barbituric acid (BA) surfaces, membrane surface charge density vs. pH of the electrolyte solution can be described using six equilibrium equations

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Summary

Introduction

Publisher’s Note: MDPI stays neutral with regard to jurisdictional claims in published maps and institutional affiliations. Up-and-coming model membrane systems which mimic the fundamental structural and functional properties of natural membranes are liposomes, those formed from phosphatidylcholine—one of the predominant lipids in the cellular membrane [3,4]. Those biomimetic systems enable the study of drug–. Perphenazine is an antipsychotic drug, a phenothiazine derivative, used to treat schizophrenia and bipolar disorders [9,10] It acts on all the levels of the central nervous system, the hypothalamus [11,12].

Chemical
Theory
Results and Discussion
Effect of Barbituric
Materials
Preparation of Liposomes Using Probe-Tip Sonication
Methods
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