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Characterization of pegylated copolymeric micelles and in vivo pharmacokinetics and biodistribution studies
Author(s) -
Lin WenJen,
Chen YiChen,
Lin ChiChang,
Chen ChauFong,
Chen JiWang
Publication year - 2006
Publication title -
journal of biomedical materials research part b: applied biomaterials
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.665
H-Index - 108
eISSN - 1552-4981
pISSN - 1552-4973
DOI - 10.1002/jbm.b.30418
Subject(s) - micelle , peg ratio , biodistribution , ethylene glycol , copolymer , chemistry , in vivo , drug carrier , amphiphile , critical micelle concentration , nuclear chemistry , drug delivery , materials science , organic chemistry , in vitro , aqueous solution , biochemistry , polymer , microbiology and biotechnology , finance , economics , biology
Abstract The aim of this study was to evaluate the influence of pegylated copolymeric micelle carrier on the biodistribution of drug in rats. The copolymers were synthesized via a modified ring‐opening copolymerization of lactone monomers (ϵ‐caprolactone, δ‐valerolactone, L ‐lactide) and poly(ethylene glycol) (PEG 10,000 and PEG 4000 ). The molecular weights and the polydispersities of synthesized copolymers were in the range of 15,000–31,000 g/mol and 1.7–2.7, respectively. All of the pegylated amphiphilic copolymers were micelles formed with low CMC values in the range of 10 −7 –10 −8 M . The drug‐loaded micelles were prepared via a dialysis method. The average particle size of micelles was around 150–200 nm. The cytotoxicity in terms of cell viability after treated with PCL–PEG, PVL–PEG, and PLA–PEG micelles was insignificant. PCL–PEG and PVL–PEG micelles without branch side chain in structures had higher drug loading than PLA–PEG micelles. In vitro release profiles indicated the release of indomethacin from these micelles exhibited a sustained release behavior. The similar phenomenon was also observed in vivo in rats. The pegylated copolymeric micelles not only decreased drug uptake by the liver and kidney, but also prolonged drug retention in the blood. © 2005 Wiley Periodicals, Inc. J Biomed Mater Res Part B: Appl Biomater, 2006