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Core‐stabilized polymeric micelle as potential drug carrier: increased solubilization of taxol
Authors:Ji‐Heung Kim  Kazunori Emoto  Michihiro Iijima  Yukio Nagasaki  Takao Aoyagi&#x;  Teruo Okano  &#x;Yasuhisa &#x;Sakurai  Kazunori Kataoka
Abstract:Poly(ethylene glycol‐b‐lactide) possessing a methoxy group at the poly(ethylene glycol) (PEG) chain end and a polymerizable methacryloyl group at the poly(lactic acid) (PLA) chain end (MeO–PEG/PLA–methacryloyl) was prepared by an anionic ring‐opening polymerization of ethylene oxide and DL ‐lactide in tandem manner initiated with a potassium 2‐methoxyethanolate, followed by end‐capping with an excess of methacrylic anhydride. The molecular weight of the obtained polymer was controlled by the initial monomer/initiator ratio, which was confirmed by the combination of gel permeation chromatography and nuclear magnetic resonance analyses. The functionality of the methacryloyl–PLA end was almost quantitative. The MeO–PEG/PLA–methacryloyl (38/35; these numbers in parentheses denote the molecular weights of PEG and PLA segments divided by 100, respectively) formed a core–shell type spherical micelle in aqueous media obtained by a dialysis technique, the cumulant diameter of which was ca. 30 nm with very low polydispersity factor. The methacryloyl group adjacent to the PLA was polymerized in the PLA core of the micelle. The polymerization proceeded thermally with radical initiator and photochemically with photo‐initiator to produce core‐polymerized nanoparticles, which was found by spectroscopic and light‐scattering techniques. Taxol‐incorporated micelles were prepared to entrap Taxol into MeO–PEG/PLA–methyacryloyl block copolymer micelles by the oil/water emulsion method. Copyright © 1999 John Wiley & Sons, Ltd.
Keywords:polymeric micelle  stable nanoparticle  drug delivery system  PEG/PLA block copolymer  micelle stability  taxol
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