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Docetaxel (DTX) is a widely used chemotherapy drug that is associated with numerous side effects and limited bioavailability. Macromolecular conjugates of DTX may improve drug targeting, solubility, reduce off-target toxicity, and overcome mechanisms of multidrug resistance. However, most polymer conjugates of DTX investigated to date make use of biopolymers, which are of fixed structure and are not well suited to optimisation and subsequent reaction to introduce further functionality. Here, we show the preparation of synthetic copolymer conjugates of DTX with drug loading of up to 20% w/w that also has potential for tuning backbone hydrophilicity and the number of reactive sites for conjugation. The intermediates produced are comprehensively characterised, as are the macromolecular conjugates, which are tested in the MCF-7 human breast adenocarcinoma cell line to assess toxicity and anticancer efficacy. The conjugates produced have IC50 values within one order of magnitude of DTX, as expected for slow release of DTX by ester hydrolysis. The results suggest that the system is promising for delivery of DTX and future work may examine conjugates of a wider molecular weight range, optimisation of DTX and PEG conjugation efficiency, and in vivo biodistribution. [ABSTRACT FROM AUTHOR]

The utility of dendrimers as effective carriers for targeted drug delivery and imaging has been facilitated by a high degree of molecular uniformity, narrow molecular weight distribution, tunable size and shape characteristics, and multivalency. Dendrimer–quantum dot (QD) nanocomposites have traditionally been synthesised by electrostatic self-assembly of preformed dendrimers and QDs, but higher generations are associated with limited flexibility and increased cytotoxicity. In this paper, we report the fabrication of CdTe QD nanoparticles using a dendronised linear copolymer bearing thiolated fourth-generation poly(amido amine) (PAMAM) dendrons as the capping and stabilising agent. We demonstrate this approach enables synthesis of nanocomposites with aqueous and photophysical stability. This paper describes the synthesis of green and yellow CdTe QD–dendronised polymer nanocomposites in situ using a partially thiolated dendronised polymer as capping agent and stabiliser. [ABSTRACT FROM AUTHOR]