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

JOURNAL OF CONTROLLED RELEASE

卷:199

Article

Pasut, Gianfranco¹  Paolino, Donatella^2,3  Celia, Christian^4,5  Mero, Anna¹  Joseph, Adrian Steve¹  Wolfram, Joy⁴  Cosco, Donato^2,3  Schiavon, Oddone¹  Shen, Haifa^4,6  Fresta, Massimo^2,3 

[1] Univ Padua, Dept Pharmaceut & Pharmacol Sci, I-35131 Padua, Italy

[2] Magna Graecia Univ Catanzaro, Dept Hlth Sci, I-88100 Catanzaro, Italy

[3] Univ Catanzaro Magna Graecia, Interreg Res Ctr Food Safety & Hlth, I-88100 Catanzaro, Italy

[4] Houston Methodist Res Inst, Dept Nanomed, Houston, TX 77030 USA

[5] Univ G dAnnunzio, Dept Pharm, I-66013 Chieti, Italy

[6] Weill Cornell Med Coll, Dept Cell & Dev Biol, New York, NY 10065 USA

关键词: Liposome;    Pegylation;    Polyethylene glycol;    Cancer therapy;    Phospholipid;   

DOI  :  10.1016/j.jconrel.2014.12.008

来源: Elsevier

【 摘 要 】

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 beta-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). (C) 2014 The Authors. Published by Elsevier B.V.

【 授权许可】

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