Institute Of Macromolecular Chemacademy Of Science Of The Czech Republicvvi Heyrovsky Sq 2162 06Prague 6Czech Republic

Institute Of Macromolecular Chemacademy Of Science Of The Czech Republicvvi Heyrovsky Sq 2162 06Prague 6Czech Republic

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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.

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