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Enhanced bioactivity of α-tocopheryl succinate based block copolymer nanoparticles by reduced hydrophobicity

(2016) MACROMOLECULAR BIOSCIENCE. 16(12). p.1824-1837
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Abstract
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 -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 -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 -tocopheryl succinate (-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 -TOS, demonstrating the importance of the hydrophilic-hydrophobic balance.
Keywords
VITAMIN-E ANALOGS, LIVING RADICAL POLYMERIZATION, DRUG-DELIVERY, 2-HYDROXYETHYL METHACRYLATE, TARGETING MITOCHONDRIA, ANTICANCER AGENTS, RAFT PROCESS, COMPLEX-II, CANCER, PEGYLATION, amphiphilic polymers, anticancer nanoparticles, HEMA, RAFT, polymerization, terpolymers, alpha-tocopheryl succinate

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Citation

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Chicago
Palao-Suay, Raquel, María Rosa Aguilar, Francisco J Parra-Ruiz, Samarendra Maji, Richard Hoogenboom, Nathan A Rohner, Susan N Thomas, and Julio San Román. 2016. “Enhanced Bioactivity of Α-tocopheryl Succinate Based Block Copolymer Nanoparticles by Reduced Hydrophobicity.” Macromolecular Bioscience 16 (12): 1824–1837.
APA
Palao-Suay, R., Rosa Aguilar, M., Parra-Ruiz, F. J., Maji, S., Hoogenboom, R., Rohner, N. A., Thomas, S. N., et al. (2016). Enhanced bioactivity of α-tocopheryl succinate based block copolymer nanoparticles by reduced hydrophobicity. MACROMOLECULAR BIOSCIENCE, 16(12), 1824–1837.
Vancouver
1.
Palao-Suay R, Rosa Aguilar M, Parra-Ruiz FJ, Maji S, Hoogenboom R, Rohner NA, et al. Enhanced bioactivity of α-tocopheryl succinate based block copolymer nanoparticles by reduced hydrophobicity. MACROMOLECULAR BIOSCIENCE. 2016;16(12):1824–37.
MLA
Palao-Suay, Raquel, María Rosa Aguilar, Francisco J Parra-Ruiz, et al. “Enhanced Bioactivity of Α-tocopheryl Succinate Based Block Copolymer Nanoparticles by Reduced Hydrophobicity.” MACROMOLECULAR BIOSCIENCE 16.12 (2016): 1824–1837. Print.
@article{8516321,
  abstract     = {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 -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 -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 -tocopheryl succinate (-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 -TOS, demonstrating the importance of the hydrophilic-hydrophobic balance.},
  author       = {Palao-Suay, Raquel and Rosa Aguilar, Mar{\'i}a and Parra-Ruiz, Francisco J and Maji, Samarendra and Hoogenboom, Richard and Rohner, Nathan A and Thomas, Susan N and San Rom{\'a}n, Julio},
  issn         = {1616-5187},
  journal      = {MACROMOLECULAR BIOSCIENCE},
  keyword      = {VITAMIN-E ANALOGS,LIVING RADICAL POLYMERIZATION,DRUG-DELIVERY,2-HYDROXYETHYL METHACRYLATE,TARGETING MITOCHONDRIA,ANTICANCER AGENTS,RAFT PROCESS,COMPLEX-II,CANCER,PEGYLATION,amphiphilic polymers,anticancer nanoparticles,HEMA,RAFT,polymerization,terpolymers,alpha-tocopheryl succinate},
  language     = {eng},
  number       = {12},
  pages        = {1824--1837},
  title        = {Enhanced bioactivity of \ensuremath{\alpha}-tocopheryl succinate based block copolymer nanoparticles by reduced hydrophobicity},
  url          = {http://dx.doi.org/10.1002/mabi.201600259},
  volume       = {16},
  year         = {2016},
}

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