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Title: Biodistribution of long-circulating PEG-Grafted nanocapsules in mice : effects of PEG chain length and density.
Authors: Mosqueira, Vanessa Carla Furtado
Legrand, Philippe
Morgat, Jean-Louis
Vert, Michel
Mysiakine, Evgueni
Gref, Ruxandra
Devissaguet, Jean-Philippe
Barratt, Gillian
Keywords: Plasma stability
Plasma clearance
Issue Date: 2001
Citation: MOSQUEIRA, V. C. F. et al. Biodistribution of long-circulating PEG-Grafted nanocapsules in mice: effects of PEG chain length and density. Pharmaceutical Research, Estados Unidos, v. 18, n.10, p. 1411-1419, 2001. Disponível em: <>. Acesso em: 20 jan. 2017.
Abstract: Purpose: To study the pharmacokinetics and biodistribution of novel polyethyleneglycol (PEG) surface-modified poly(rac-lactide) (PLA) nanocapsules (NCs) and to investigate the influence of PEG chain length and content. Methods: The biodistribution and plasma clearance in mice of different NC formulations were studied with [3H]-PLA. PLA-PEG copolymers were used in NC preparations at different chain lengths (5 kDa and 20 kDa) and PEG contents (10% and 30% w/w of total polymer). In vitro and in vivo stability were also checked. Results: Limited [3H]-PLA degradation was observed after incubation in mouse plasma for 1 h, probably because of to the large surface area and thin polymer wall. After injection into mice, NCs prepared with PLA-PEG copolymers showed an altered distribution compared to poloxamer-coated PLA NCs. An increased concentration in plasma was also observed for PLA-PEG NCs, even after 24 h. A dramatic difference in the pharmacokinetic parameters of PLA-PEG 45–20 30% NCs compared to poloxamer-coated NCs indicates that covalent attachment, longer PEG chain lengths, and higher densities are necessary to produce an increased half-life of NCs in vivo. Conclusions: Covalently attached PEG on the surface of NCs substantially can reduce their clearance from the blood compartment and alter their biodistribution.
ISSN: 1573-904X 
Appears in Collections:DEFAR - Artigos publicados em periódicos

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