Polyethylene glycol (PEG)-dendron phospholipids as innovative constructs for the preparation of super stealth liposomes for anticancer therapy

Gianfranco Pasut, Donatella Paolino, Christian Celia, Anna Mero, Adrian Steve Joseph, Joy Wolfram, Donato Cosco, Oddone Schiavon, Haifa Shen, Massimo Fresta

Research output: Contribution to journalArticle

79 Scopus citations

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).

Original languageEnglish (US)
Pages (from-to)106-113
Number of pages8
JournalJournal of Controlled Release
Volume199
DOIs
StatePublished - Feb 10 2015

Keywords

  • Cancer therapy
  • Liposome
  • Pegylation
  • Phospholipid
  • Polyethylene glycol

ASJC Scopus subject areas

  • Pharmaceutical Science

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