The effect of different surface chemical groups on drug binding to liposomes

摘要: The binding of four secondary and tertiary amine drugs with local anesthetic activity (propranolol, tetracaine, lidocaine, procaine) to liposomes containing charged surface groups different chemical composition has been investigated. Binding is determined by measurement partition coefficients drug induced zeta potential changes the liposomes. For propranolol 30% total amount dissolved in phosphatidylcholine located as protonated form liposome surface. Fifty percent tetracaine 13% procaine contribute charges. Negative charges (phosphatidylserine) facilitate protonization Positive (hexadecyltrimethylammonium) prevent drugs. Different single negatively phospholipids or electrostatically neutral lipids have no significant effect on which proves that not influenced steric bulky head group configurations. interact hydrophobically lipid phase such a way protonizes presence phosphate oxygen phospholipid. Hexadecanoic acid deeper within than other phospholipids. Correspondingly action weaker prevented.