Incorporation of simvastatin into lipid membranes: Why deliver a statin in form of inclusion complex with hydrophilic cyclodextrin

In this work, the effects of simvastatin (SIM), (2-hydroxypropyl)-?-cyclodextrin (HP?CD) and their complex (SIM:HP?CD) on structure properties lipid membranes were investigated for first time by Langmuir technique combined with PM-IRRAS spectroscopy. An improved understanding differences interactions between free SIM, SIM in form an inclusion HP?CD membrane will improve development preparation methods vivo applications. Monolayers 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC), cholesterol (Chol) mixture DMPC:Chol (7:3) served as simple models one leaflet cell membrane. The penetration well-organized layers lead to fluidization but extent unwanted effect was smaller when drug delivered SIM:HP?CD complex. Surface pressure vs. dependencies showed that encapsulated cyclodextrin dissociated from upon contact layer weak exterior polar part headgroups facilitated smooth incorporation released lipophilic into At a longer time-scale, ligand removed some cholesterol, not DMPC, layer, hence, similarly enzyme inhibiting action statins – it decrease amount Delivery is proposed approach improving its bioavailability cholesterol-lowering therapies.