title: Aqueous-core PEG-coated PLA nanocapsules for an efficient entrapment of water soluble anticancer drugs and a smart therapeutic response.
abstract: Novel PEGylated PLA nanocapsules (PEG-AcPLA nanocapsules), loading high percentage of water soluble drugs have been formulated by using multiple emulsion technique without using conventional stabilizers. In particular, sodium deoxycholate hydrate has been used to obtain nanocapsules having a mean diameter of about 200 nm and a polydispersity index of ∼ 0.1. Gemcitabine hydrochloride (GEM) was used as a model of hydrophilic drug. GEM-loaded PEG-AcPLA nanocapsules demonstrated a high encapsulation efficacy and the drug-release followed a zero-order kinetic. MTT-assay evidenced an increased antitumor effect of GEM-loaded PEG-AcPLA nanocapsules compared to the free drug on different cancer cell lines and confocal laser scanning microscopy showed a significant improvement of cell interaction at 6h of incubation. In vivo anticancer activity of GEM-loaded PEG-AcPLA nanocapsules using two xenograft murine models of human solid tumors further supported the efficacy of this nano-drug, thus providing preliminary results about the potential clinical application of this innovative nanotherapeutic.
authors.affiliation: Department of Health Sciences, University "Magna Græcia" of Catanzaro, Catanzaro, Italy; Univ Paris-Sud, Institut Galien Paris-Sud, UMR CNRS 8612, LabEx LERMIT, Faculté de pharmacie, Châtenay-Malabry Cedex, France.
authors.forename: Donato
authors.initials: D
authors.lastname: Cosco
authors.affiliation: Department of Health Sciences, University "Magna Græcia" of Catanzaro, Catanzaro, Italy; IRC FSH-Interregional Research Center for Food Safety & Health, University of Catanzaro "Magna Græcia", Catanzaro, Italy.
authors.forename: Donatella
authors.initials: D
authors.lastname: Paolino
authors.affiliation: Nanostructures Department, Istituto Italiano di Tecnologia (IIT), Genova, Italy.
authors.forename: Francesco
authors.initials: F
authors.lastname: De Angelis
authors.affiliation: Department of Health Sciences, University "Magna Græcia" of Catanzaro, Catanzaro, Italy.
authors.forename: Felisa
authors.initials: F
authors.lastname: Cilurzo
authors.affiliation: Department of Pharmacy, University of Chieti-Pescara "G. d'Annunzio", Chieti, Italy; Department of Nanomedicine, Houston Methodist Research Institute, Houston, USA.
authors.forename: Christian
authors.initials: C
authors.lastname: Celia
authors.affiliation: Department of Pharmacy, University of Chieti-Pescara "G. d'Annunzio", Chieti, Italy.
authors.forename: Luisa
authors.initials: L
authors.lastname: Di Marzio
authors.affiliation: Department of Health Sciences, University "Magna Græcia" of Catanzaro, Catanzaro, Italy.
authors.forename: Diego
authors.initials: D
authors.lastname: Russo
authors.affiliation: Univ Paris-Sud, Institut Galien Paris-Sud, UMR CNRS 8612, LabEx LERMIT, Faculté de pharmacie, Châtenay-Malabry Cedex, France; CNRS, UMR 8612, Chatenay-Malabry Cedex, France.
authors.forename: Nicolas
authors.initials: N
authors.lastname: Tsapis
authors.affiliation: Univ Paris-Sud, Institut Galien Paris-Sud, UMR CNRS 8612, LabEx LERMIT, Faculté de pharmacie, Châtenay-Malabry Cedex, France; CNRS, UMR 8612, Chatenay-Malabry Cedex, France. Electronic address: elias.fattal@u-psud.fr.
authors.forename: Elias
authors.initials: E
authors.lastname: Fattal
authors.affiliation: Department of Health Sciences, University "Magna Græcia" of Catanzaro, Catanzaro, Italy; IRC FSH-Interregional Research Center for Food Safety & Health, University of Catanzaro "Magna Græcia", Catanzaro, Italy. Electronic address: fresta@unicz.it.
authors.forename: Massimo
authors.initials: M
authors.lastname: Fresta
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry*; D045744:Cell Line, Tumor; D003841:Deoxycytidine / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000737:chemistry; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry; D005260:Female; D019073:HT29 Cells; D006801:Humans; D051379:Mice; D016688:Mice, Inbred NOD; D016513:Mice, SCID; D053769:Nanocapsules / Q000008:administration & dosage* / Q000737:chemistry*; D010316:Particle Size; D011092:Polyethylene Glycols / Q000008:administration & dosage* / Q000737:chemistry*; D012995:Solubility; D014867:Water / Q000737:chemistry*; D000093542:Gemcitabine
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D053769:Nanocapsules; C542623:monomethoxypolyethyleneglycol-polylactide block copolymer; D014867:Water; D003841:Deoxycytidine; D011092:Polyethylene Glycols; D000093542:Gemcitabine
keywords: Aqueous core; Gemcitabine; PLA nanocapsules; Turbiscan lab; Water-soluble anticancer drugs; Xenograft models