Cellular and endosomal lipid bilayers

Cellular and endosomal lipid bilayers are fundamental structural components of eukaryotic cells, consisting primarily of a double layer of phospholipids interspersed with proteins and cholesterol. They serve as selective barriers that regulate the passage of ions and molecules, maintaining cellular homeostasis and facilitating compartmentalization (StatPearls, 2023). In pharmacology, these bilayers are critical targets for antimicrobial agents, such as Amphotericin B and Daptomycin, which disrupt membrane integrity to induce cell death in pathogens (PubMed, PMID: 23027178). Furthermore, they are central to the efficacy of modern drug delivery systems like lipid nanoparticles (LNPs); these systems interact with endosomal membranes to facilitate the cytosolic delivery of nucleic acids through endosomal escape (Nature Reviews Drug Discovery, 2021). Dysregulation of membrane composition or trafficking is implicated in various pathologies, including viral infections, where pathogens exploit these bilayers for entry, and respiratory distress syndrome, where surfactant deficiency leads to alveolar collapse (NIH, 2022).

Other names

Biological membranesPlasma membraneEndosomal membranePhospholipid bilayerCytoplasmic membrane

Drugs targeting lipid bilayers typically act through pore formation, physical disruption of membrane integrity, alteration of membrane fluidity, or by facilitating endosomal escape via membrane fusion or the proton sponge effect. In the case of surfactants, they reduce surface tension at the air-liquid interface of the alveoli.