title: Microcalorimetric and zeta potential study on binding of drugs on liposomes.
abstract: In this work, isothermal titration calorimetry (ITC) combined with zeta potential measurements was used to study the binding and partitioning of three beta-blockers, alprenolol, labetalol and propranolol, and the local anaesthetic tetracaine into liposomes. The thermodynamic parameters of enthalpy, entropy, the Gibbs energy and the binding constant were determined using the one site model. Furthermore, the binding constants corrected for the electrostatic contribution were used to assess the partition coefficients for the drugs. Also, the effect of the concentration, ionic strength, temperature and membrane curvature on the interaction was included in the evaluation.
authors.affiliation: Aalto University, School of Science and Technology, Department of Chemistry, PO Box 16100, FI-00076 Aalto, Finland.
authors.forename: Marjukka
authors.initials: M
authors.lastname: Ikonen
authors.forename: Lasse
authors.initials: L
authors.lastname: Murtomäki
authors.forename: Kyösti
authors.initials: K
authors.lastname: Kontturi
mesh_terms: D000465:Algorithms; D000526:Alprenolol / Q000737:chemistry / Q000378:metabolism; D001665:Binding Sites; D001667:Binding, Competitive; D002151:Calorimetry / Q000379:methods*; D019277:Entropy; D007700:Kinetics; D007741:Labetalol / Q000737:chemistry / Q000378:metabolism; D008081:Liposomes / Q000737:chemistry* / Q000378:metabolism; D008956:Models, Chemical; D015394:Molecular Structure; D004364:Pharmaceutical Preparations / Q000737:chemistry* / Q000378:metabolism; D010713:Phosphatidylcholines / Q000737:chemistry; D010715:Phosphatidylglycerols / Q000737:chemistry; D011433:Propranolol / Q000737:chemistry / Q000378:metabolism; D013748:Tetracaine / Q000737:chemistry / Q000378:metabolism; D013816:Thermodynamics
chemical_list: D008081:Liposomes; D004364:Pharmaceutical Preparations; D010713:Phosphatidylcholines; D010715:Phosphatidylglycerols; D013748:Tetracaine; C060037:1-palmitoyl-2-oleoylglycero-3-phosphoglycerol; D000526:Alprenolol; D011433:Propranolol; D007741:Labetalol; C028694:1-palmitoyl-2-oleoylphosphatidylcholine