title: Polyethylene glycol (PEG)-dendron phospholipids as innovative constructs for the preparation of super stealth liposomes for anticancer therapy.
abstract: Pegylation of nanoparticles has been widely implemented in the field of drug delivery to prevent macrophage clearance and increase drug accumulation at a target site. However, the shielding effect of polyethylene glycol (PEG) is usually incomplete and transient, due to loss of nanoparticle integrity upon systemic injection. Here, we have synthesized unique PEG-dendron-phospholipid constructs that form super stealth liposomes (SSLs). A β-glutamic acid dendron anchor was used to attach a PEG chain to several distearoyl phosphoethanolamine lipids, thereby differing from conventional stealth liposomes where a PEG chain is attached to a single phospholipid. This composition was shown to increase liposomal stability, prolong the circulation half-life, improve the biodistribution profile and enhance the anticancer potency of a drug payload (doxorubicin hydrochloride).
authors.affiliation: Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padua 35131, Italy.
authors.forename: Gianfranco
authors.initials: G
authors.lastname: Pasut
authors.affiliation: Department of Health Science, University "Magna Græcia" of Catanzaro, Catanzaro 88100, Italy; Interregional Research Center for Food Safety & Health, University of Catanzaro "Magna Græcia", Catanzaro 88100, Italy.
authors.forename: Donatella
authors.initials: D
authors.lastname: Paolino
authors.affiliation: Department of Nanomedicine, Houston Methodist Research Institute, Houston, TX 77030, USA; Department of Pharmacy, University "G. D'Annunzio" of Chieti-Pescara, Chieti 66013, Italy.
authors.forename: Christian
authors.initials: C
authors.lastname: Celia
authors.affiliation: Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padua 35131, Italy.
authors.forename: Anna
authors.initials: A
authors.lastname: Mero
authors.affiliation: Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padua 35131, Italy.
authors.forename: Adrian Steve
authors.initials: AS
authors.lastname: Joseph
authors.affiliation: Department of Nanomedicine, Houston Methodist Research Institute, Houston, TX 77030, USA.
authors.forename: Joy
authors.initials: J
authors.lastname: Wolfram
authors.affiliation: Department of Health Science, University "Magna Græcia" of Catanzaro, Catanzaro 88100, Italy; Interregional Research Center for Food Safety & Health, University of Catanzaro "Magna Græcia", Catanzaro 88100, Italy.
authors.forename: Donato
authors.initials: D
authors.lastname: Cosco
authors.affiliation: Department of Pharmaceutical and Pharmacological Sciences, University of Padua, Padua 35131, Italy.
authors.forename: Oddone
authors.initials: O
authors.lastname: Schiavon
authors.affiliation: Department of Nanomedicine, Houston Methodist Research Institute, Houston, TX 77030, USA; Department of Cell and Developmental Biology, Weill Cornell Medical College, New York, NY 10065, USA.
authors.forename: Haifa
authors.initials: H
authors.lastname: Shen
authors.affiliation: Department of Health Science, University "Magna Græcia" of Catanzaro, Catanzaro 88100, Italy; Interregional Research Center for Food Safety & Health, University of Catanzaro "Magna Græcia", Catanzaro 88100, Italy. Electronic address: fresta@unicz.it.
authors.forename: Massimo
authors.initials: M
authors.lastname: Fresta
mesh_terms: D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000493:pharmacokinetics / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D018938:Caco-2 Cells; D050091:Dendrimers; D004317:Doxorubicin / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology; D016503:Drug Delivery Systems; D015195:Drug Design; D004355:Drug Stability; D006801:Humans; D008051:Lipid Bilayers; D008081:Liposomes / Q000737:chemistry*; D051379:Mice; D008807:Mice, Inbred BALB C; D010743:Phospholipids / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry*; D014018:Tissue Distribution
chemical_list: D000903:Antibiotics, Antineoplastic; D000970:Antineoplastic Agents; D050091:Dendrimers; D008051:Lipid Bilayers; D008081:Liposomes; D010743:Phospholipids; D011092:Polyethylene Glycols; D004317:Doxorubicin
keywords: Cancer therapy; Liposome; Pegylation; Phospholipid; Polyethylene glycol