title: Preparation and characterisation of the colistin-entrapped liposome driven by electrostatic interaction for intravenous administration.
abstract: Potential use of liposome for polycationic colistin is hindered by their phospholipid membrane permeability. In this study, liposomes were modified with sodium cholesteryl sulphate (Chol-SO4(-)) for improving the colistin loading by enhancing the colistin-bilayer electrostatic attraction. We have evaluated two liposomes: colistin-entrapped liposome of Chol-SO4(-) (CCL) and coated Chol-SO4(-)/colistin complex liposome (CCCL). In comparison with CCL which formed large aggregates at Chol-SO4(-)/colistin charge ratio below 2:1, CCCL showed a smaller size less dependent on the charge ratio, probably arising from more colistin entrapped on the inner leaflet of bilayer. Both liposomes exhibited significantly increased entrapment efficiency as compared with the liposome without Chol-SO4(-). But colistin released upon dilution, implying free transfer of colistin through bilayers. Pharmacokinetics results showed the approximately four-fold increase in the plasma AUC0-8 h for CCCL and CCL as compared with colistin solution, showing potential benefit for infectious target localisation by prolonging the systemic circulation of colistin.
authors.affiliation: a Department of Pharmaceutics , School of Pharmacy, Shenyang Pharmaceutical University , Shenyang , China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Li
authors.affiliation: a Department of Pharmaceutics , School of Pharmacy, Shenyang Pharmaceutical University , Shenyang , China.
authors.forename: Lingling
authors.initials: L
authors.lastname: Huang
authors.affiliation: a Department of Pharmaceutics , School of Pharmacy, Shenyang Pharmaceutical University , Shenyang , China.
authors.forename: Chengcheng
authors.initials: C
authors.lastname: Tang
authors.affiliation: a Department of Pharmaceutics , School of Pharmacy, Shenyang Pharmaceutical University , Shenyang , China.
authors.forename: Enbo
authors.initials: E
authors.lastname: Zhang
authors.affiliation: a Department of Pharmaceutics , School of Pharmacy, Shenyang Pharmaceutical University , Shenyang , China.
authors.forename: Lei
authors.initials: L
authors.lastname: Ding
authors.affiliation: a Department of Pharmaceutics , School of Pharmacy, Shenyang Pharmaceutical University , Shenyang , China.
authors.forename: Li
authors.initials: L
authors.lastname: Yang
mesh_terms: D061605:Administration, Intravenous; D000818:Animals; D002788:Cholesterol Esters / Q000737:chemistry* / Q000494:pharmacology*; D003091:Colistin / Q000737:chemistry* / Q000494:pharmacology*; D008081:Liposomes; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D055672:Static Electricity
chemical_list: D002788:Cholesterol Esters; D008081:Liposomes; C007045:cholesteryl sulfate; D003091:Colistin
keywords: Liposome; colistin; electrostatic interaction; pharmacokinetics; sodium cholesteryl sulphate