Journal
BIOCHIMICA ET BIOPHYSICA ACTA-BIOMEMBRANES
Volume 1768, Issue 3, Pages 737-743Publisher
ELSEVIER SCIENCE BV
DOI: 10.1016/j.bbamem.2006.12.005
Keywords
long-circulating liposomes; pharmacokinetics; poly(ethylene glycol); poly(amino acid)s; accelerated blood clearance; repeated administration
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'Stealth' liposomes with a poly(ethylenc glycol) (PEG) coating are frequently studied for drug delivery and diagnostic purposes because of their prolonged blood circulation kinetics. However, several recent reports have demonstrated that PEG-liposomes are rapidly cleared at single low lipid doses (< 1 mu mol/kg) and upon repeated administration (time interval between the injections 5 days-4 weeks). Recently, poly(amino acid)based stealth liposome coatings have been developed as alternative to the PEG-coating. In this study, the pharmacokinetic behavior of liposomes coated with the poly(amino acid) poly(hydroxyethyl-L-asparagine) (PHEA) was evaluated at low lipid doses and upon repeated administration in rats. Blood circulation times and hepatosplenic localization of PHEA-liposomes were assessed after intravenous injection. When administered at a dose of 0.25 mu mol/kg or less, PHEA-liposomes showed significantly longer blood circulation times than PEG-liposomes. A second dose of PHEA-liposomes I week after the first injection was less rapidly cleared from the circulation than a second dose of PEG-liposomes. Although the mechanisms behind these observations are still not clear yet, the use of PHEA-liposomes appears beneficial when single low lipid doses and/or repeated dosing schedules are being applied. (c) 2006 Elsevier B.V. All rights reserved.
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