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Chytil P.,Institute Of Macromolecular Chemacademy Of Science Of The Czech Republicvvi Heyrovsky Sq 2162 06Prague 6Czech Republic | Koziolova E.,Institute Of Macromolecular Chemacademy Of Science Of The Czech Republicvvi Heyrovsky Sq 2162 06Prague 6Czech Republic | Janouskova O.,Institute Of Macromolecular Chemacademy Of Science Of The Czech Republicvvi Heyrovsky Sq 2162 06Prague 6Czech Republic | Kostka L.,Institute Of Macromolecular Chemacademy Of Science Of The Czech Republicvvi Heyrovsky Sq 2162 06Prague 6Czech Republic | And 2 more authors.
Macromolecular Bioscience | Year: 2015

High-molecular-weight star polymer drug nanocarriers intended for the treatment and/or visualisation of solid tumours were synthesised, and their physico-chemical and preliminary in vitro biological properties were determined. The water-soluble star polymer carriers were prepared by the grafting of poly(amido amine) (PAMAM) dendrimers by hetero-telechelic N-(2-hydroxypropyl)methacrylamide (HPMA) copolymers, synthesised by the controlled radical Reversible Addition Fragmentation chain Transfer (RAFT) polymerisation. The well-defined star copolymers with Mw values ranging from 2·105 to 6·105 showing a low dispersity (approximately 1.2) were prepared in a high yield. A model anticancer drug, doxorubicin, was bound to the star polymer through a hydrazone bond, enabling the pH-controlled drug release in the target tumour tissue. The activated polymer arm ends of the star copolymer carrier enable a one-point attachment for the targeting ligands and/or a labelling moiety. In this study, the model TAMRA fluorescent dye was used to prove the feasibility of the polymer carrier visualisation by optical imaging in vitro. The tailor-made structure of the star polymer carriers should facilitate the synthesis of targeted polymer-drug conjugates, even polymer theranostics, for simultaneous tumour drug delivery and imaging. © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim. Source

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