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pH‐Responsive Flower‐Type Micelles Formed by a Biotinylated Poly(2‐vinylpyridine)‐block‐poly(ethylene oxide)‐block‐poly(ε‐caprolactone) Triblock Copolymer
Authors:Kathy Van Butsele  Sébastien Cajot  Sandra Van Vlierberghe  Peter Dubruel  Catherine Passirani  Jean‐Pierre Benoit  Robert Jérôme  Christine Jérôme
Affiliation:1. Center for Education and Research on Macromolecules (CERM) University of Liège B6 Sart‐Tilman, 4000 Liege (Belgium);2. Polymer Chemistry & Biomaterials Research Group University of Gent Krijgslaan 281, 9000 Gent (Belgium);3. INSERM U 646 University of Angers Rue A. Boquel 10, 49100 Angers (France)
Abstract:In the present work, a method is proposed to assemble pH‐responsive, flower‐like micelles that can expose a targeting unit at their periphery upon a decrease in pH. The micelles are composed of a novel biotinylated triblock copolymer of poly(εε‐caprolactone)‐block‐poly(ethylene oxide)‐block‐poly(2‐vinylpyridine) (PCL‐b‐PEO‐b‐P2VP) and the non‐biotinylated analogue. The block copolymers are synthesized by sequential anionic and ring‐opening polymerization. The pH‐dependent micellization behaviour in aqueous solution of the triblock copolymers developed is studied using dynamic light scattering, zeta potential, transmission electron microscopy (TEM), and fluorimetric measurements. The shielding of the biotin at neutral pH and their availability at the micelle surface upon protonation is established by TEM and surface plasmon resonance with avidin and streptavidin‐coated gold surfaces. The preliminary stealthy behavior of these pH‐responsive micelles is examined using the complement activation (CH50) test.
Keywords:block copolymer micelles  colloidal particles  drug delivery
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