Effective anticancer therapy can be achieved by designing a targeted drug-delivery system
with high stability during circulation and efficient uptake by the target tumour cancer cells.
We report here a novel nano-assembled drug-delivery system, formed by multivalent
host–guest interactions between a polymer–cyclodextrin conjugate and a polymer–paclitaxel
conjugate. The multivalent inclusion complexes confer high stability to the nano-assembly,
which efficiently delivers paclitaxel into the targeted cancer cells via both passive and active
targeting mechanisms. The ester linkages between paclitaxel and the polymer backbone
permit efficient release of paclitaxel within the cell by degradation. This novel targeted
nano-assembly exhibits significant antitumour activity in a mouse tumour model. The
strategy established in this study also provides knowledge for the development of advanced
anticancer drug delivery.