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

Carbohydr Res. 2015 Aug 14:412:7-14. doi: 10.1016/j.carres.2015.04.021. Epub 2015 May 5.

Abstract

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.

Keywords: Artesunate; Characterization; Cyclodextrin; Cytotoxicity; Polyrotaxane; Synthesis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemical synthesis
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / toxicity
  • Artemisinins / administration & dosage*
  • Artemisinins / chemical synthesis
  • Artemisinins / toxicity
  • Artesunate
  • Calorimetry, Differential Scanning
  • Cell Line, Tumor
  • Colonic Neoplasms / metabolism
  • Cyclodextrins / chemical synthesis*
  • Cyclodextrins / chemistry*
  • Cyclodextrins / toxicity
  • Drug Delivery Systems*
  • Drug Evaluation*
  • Humans
  • Magnetic Resonance Imaging
  • Poloxamer / chemical synthesis*
  • Poloxamer / chemistry*
  • Poloxamer / toxicity
  • Rotaxanes / chemical synthesis*
  • Rotaxanes / chemistry*
  • Rotaxanes / toxicity
  • X-Ray Diffraction

Substances

  • Antineoplastic Agents
  • Artemisinins
  • Cyclodextrins
  • Rotaxanes
  • polyrotaxane
  • Poloxamer
  • Artesunate
  • artenimol