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

J Control Release

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:

Published: February 2015


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Article 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).

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http://dx.doi.org/10.1016/j.jconrel.2014.12.008DOI Listing

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