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Enhanced Bioactivity of α‐Tocopheryl Succinate Based Block Copolymer Nanoparticles by Reduced Hydrophobicity
Author(s) -
PalaoSuay Raquel,
Aguilar María Rosa,
ParraRuiz Francisco J.,
Maji Samarendra,
Hoogenboom Richard,
Rohner Nathan A.,
Thomas Susan N.,
Román Julio San
Publication year - 2016
Publication title -
macromolecular bioscience
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.924
H-Index - 105
eISSN - 1616-5195
pISSN - 1616-5187
DOI - 10.1002/mabi.201600259
Subject(s) - copolymer , amphiphile , ethylene glycol , polymerization , chain transfer , macromolecule , polymer , chemistry , polymer chemistry , nanoparticle , methacrylate , peg ratio , reversible addition−fragmentation chain transfer polymerization , radical polymerization , materials science , chemical engineering , organic chemistry , nanotechnology , engineering , biochemistry , finance , economics
Well‐structured amphiphilic copolymers are necessary to obtain self‐assembled nanoparticles (NPs) based on synthetic polymers. Highly homogeneous and monodispersed macromolecules obtained by controlled polymerization have successfully been used for this purpose. However, disaggregation of the organized macromolecules is desired when a bioactive element, such as α‐tocopheryl succinate, is introduced in self‐assembled NPs and this element must be exposed or released to exert its action. The aim of this work is to demonstrate that the bioactivity of synthetic NPs based on defined reversible addition‐fragmentation chain transfer polymerization copolymers can be enhanced by the introduction of hydrophilic comonomers in the hydrophobic segment. The amphiphilic terpolymers are based on poly(ethylene glycol) (PEG) as hydrophilic block, and a hydrophobic block based on a methacrylic derivative of α‐tocopheryl succinate (MTOS) and small amounts of 2‐hydroxyethyl methacrylate (HEMA) (PEG‐ b ‐poly(MTOS‐ co ‐HEMA)). The introduction of HEMA reduces hydrophobicity and introduces “disorder” both in the homogeneous blocks and the compact core of the corresponding NPs. These NPs are able to encapsulate additional α‐tocopheryl succinate (α‐TOS) with high efficiency and their biological activity is much higher than that described for the unmodified copolymers, proposedly due to more efficient degradation and release of α‐TOS, demonstrating the importance of the hydrophilic–hydrophobic balance.