INTERACTION OF COLISTIN WITH LIPIDS IN LIPOSOMES AND MONOLAYERS

Citation
C. Mestres et al., INTERACTION OF COLISTIN WITH LIPIDS IN LIPOSOMES AND MONOLAYERS, International journal of pharmaceutics, 160(1), 1998, pp. 99-107
Citations number
15
Categorie Soggetti
Pharmacology & Pharmacy
ISSN journal
03785173
Volume
160
Issue
1
Year of publication
1998
Pages
99 - 107
Database
ISI
SICI code
0378-5173(1998)160:1<99:IOCWLI>2.0.ZU;2-6
Abstract
Colistin is an antibiotic member of the polymixin family, showing a hi gh amphipathic character. Its mechanism of action has been related to its ability to disrupt phospholipid bilayers of the bacterial membrane . Due to its hydrophobic properties colistin can interact both with th e polar heads and the alkyl chains of the phospholipids. Moreover, it has a polycationic structure, so its interactions with phospholipids s hould be highly dependent on the electric charge of the lipid and the ionisation state of polymixin molecule. In the present paper we report on physicochemical studies to define the type and characteristics of these interactions. The surface activity of colistin has been shown to be highly dependent on the pH of the medium, the less protonated form s being more stable at the air-water interface. Interaction with phosp holipid monolayers shows the same tendency. Colistin is also able to f orm mixed monolayers with phospholipids with small deviations from ide ality. Physicochemical studies carried out with fluorescent probes ind icate the presence of pure colistin aggregates that can coexist with m ixed micelles composed of colistin/phospholipids. In no case did the i nteraction cause significative changes in the transition temperature o f phospholipids. (C) 1998 Elsevier Science B.V.