title: Surface functionalizing of a lipid nanosystem to promote brain targeting: step-by-step design and physico-chemical characterization.
abstract: The use of lipid nanosystems as drug delivery to the central nervous system may be advantageous over the current strategies. The aim of this study was to develop and characterize functionalized liposomes for treatment of brain diseases. The covalent method of coupling IgG to liposomes via the derivatized lipid 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine-N-[4-(p-maleimidophenyl)butyramide](MPB-PE) was investigated. Optimized coupling conditions are shown to result in the efficient conjugation of IgG to liposomes containing low concentrations of MPB-PE (3/1 SH:IgG). The qualitative analysis has shown that after the extrusion process, more homogeneous populations of vesicles have been obtained with a nanometric size suitable to be effective to further anchor the protein. Negative values of zeta potential demonstrate that they are stable systems. Lyophilization was used to maintain the stability of the formulation. These very interesting results encourage further investigations to formulate peptide- and protein-loaded immunoliposomes, making targeting of liposomes as an attractive approach for brain drug delivery.
authors.affiliation: a Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy , Universidad de Sevilla , Seville , Spain and.
authors.forename: M J
authors.initials: MJ
authors.lastname: Cózar-Bernal
authors.affiliation: a Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy , Universidad de Sevilla , Seville , Spain and.
authors.forename: E
authors.initials: E
authors.lastname: García-Esteban
authors.affiliation: b Institute of Materials Science of Seville, Spanish National Research Council (CSIC), Universidad de Sevilla , Seville , Spain.
authors.forename: P J
authors.initials: PJ
authors.lastname: Sánchez-Soto
authors.affiliation: a Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy , Universidad de Sevilla , Seville , Spain and.
authors.forename: A M
authors.initials: AM
authors.lastname: Rabasco
authors.affiliation: a Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy , Universidad de Sevilla , Seville , Spain and.
authors.forename: M L
authors.initials: ML
authors.lastname: González-Rodríguez
mesh_terms: D001921:Brain / Q000187:drug effects*; D001927:Brain Diseases / Q000188:drug therapy; D002626:Chemistry, Pharmaceutical / Q000379:methods; D016503:Drug Delivery Systems / Q000379:methods; D007074:Immunoglobulin G / Q000737:chemistry; D008055:Lipids / Q000737:chemistry*; D008081:Liposomes / Q000008:administration & dosage / Q000737:chemistry; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry*; D010316:Particle Size; D010714:Phosphatidylethanolamines / Q000737:chemistry
chemical_list: D007074:Immunoglobulin G; D008055:Lipids; D008081:Liposomes; D010714:Phosphatidylethanolamines; C033182:N-(4-(4-maleimidophenyl)butyryl)phosphatidylethanolamine
keywords: Blood brain barrier; molecular Trojan Horse; targeted drug delivery