title: Doxorubicin-loaded galactose-conjugated poly(d,l-lactide-co-glycolide) nanoparticles as hepatocyte-targeting drug carrier.
abstract: The objective of this work is to produce doxorubicin-loaded galactose-conjugated poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles (NPs) to be specifically recognised by human hepatoma cellular carcinoma (Hep G2) cells and assess NPs cytotoxicity. Doxorubicin-unloaded and doxorubicin-loaded galactose-conjugated PLGA NPs were prepared using an emulsion method and characterised for morphology, size, drug release behaviour, Hep G2 recognition and cell cytotoxicity. The produced doxorubicin-loaded PLGA-galactose-conjugate nanoparticles (PLGA-GAL NPs) are spherical in shape with a size of 365 ± 74 nm, a drug encapsulation efficiency of 69% and released in a biphasic pattern with higher release rates at pH 5. In vitro cell studies confirmed the specific interaction between the receptors of Hep G2 and the PLGA-GAL NPs. Cell cytotoxicity tests showed that unloaded NPs are non-toxic and that doxorubicin-loaded NPs caused a cellular viability decrease of around 80%, therefore representing a promising approach to improve liver-specific drug delivery.
authors.affiliation: a LAQV, REQUIMTE, Departamento de Química , Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa , Caparica , Portugal ;
authors.forename: M
authors.initials: M
authors.lastname: Margarida Cardoso
authors.affiliation: a LAQV, REQUIMTE, Departamento de Química , Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa , Caparica , Portugal ;
authors.forename: Inês N
authors.initials: IN
authors.lastname: Peça
authors.affiliation: a LAQV, REQUIMTE, Departamento de Química , Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa , Caparica , Portugal ;
authors.forename: Cláudia D
authors.initials: CD
authors.lastname: Raposo
authors.affiliation: a LAQV, REQUIMTE, Departamento de Química , Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa , Caparica , Portugal ;
authors.forename: Krasimira T
authors.initials: KT
authors.lastname: Petrova
authors.affiliation: a LAQV, REQUIMTE, Departamento de Química , Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa , Caparica , Portugal ;
authors.forename: M
authors.initials: M
authors.lastname: Teresa Barros
authors.affiliation: a LAQV, REQUIMTE, Departamento de Química , Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa , Caparica , Portugal ;|b Instituto Gulbenkian de Ciência , Oeiras , Portugal.
authors.forename: Rui
authors.initials: R
authors.lastname: Gardner
authors.affiliation: a LAQV, REQUIMTE, Departamento de Química , Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa , Caparica , Portugal ;|b Instituto Gulbenkian de Ciência , Oeiras , Portugal.
authors.forename: A
authors.initials: A
authors.lastname: Bicho
mesh_terms: D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D004317:Doxorubicin / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology; D005690:Galactose / Q000737:chemistry*; D056945:Hep G2 Cells; D022781:Hepatocytes / Q000378:metabolism*; D006801:Humans; D053758:Nanoparticles / Q000737:chemistry*; D011098:Polyglactin 910 / Q000737:chemistry*
chemical_list: D004337:Drug Carriers; D011098:Polyglactin 910; D004317:Doxorubicin; D005690:Galactose
keywords: Galactosylated PLGA; Hep G2 cells; asialoglycoprotein receptor (ASPGR); doxorubicin delivery; liver-specific nanoparticles