Synthesis, characterization and in vitro evaluation of a series of novel polyrotaxane-based delivery system for artesunate

• A series of novel artesunate-polyrotaxanes (ATS-PRs) were prepared and characterized.
• The ATS-PRs had higher antiproliferative activities than free ATS and DHA.
• The ATS-PRs are potentially useful for their application on human colon cancer chemotherapies.

A series of novel artesunate-polyrotaxanes (ATS-PRs) with folic acid capped, in which artesunate (ATS) was covalently bound to a cyclodextrin (CD) of the polyrotaxane (PR), were synthesized and were characterized by NMR, XRD, TG and DSC. The cytotoxicities of ATS-PRs on human colon cancer cell lines HT-29, SW480, HTC116 and DLD-1 showed that their antitumor activities were better than that of artesunate (ATS) and dihydroartemisinin (DHA). These ATS-PRs may provide a useful approach to the development of a highly effective drug candidate for the chemotherapy of human colon cancer.

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