A novel polyrotaxane-based delivery system for scutellarin: preparation, characterization, and in vitro evaluation

Carbohydr Res. 2013 Oct 18:380:149-55. doi: 10.1016/j.carres.2013.07.009. Epub 2013 Jul 29.

Abstract

The safe and effective polyrotaxane-based drug delivery system could potentially increase the antiproliferative activity of antitumor medicine. A novel scutellarin-polyrotaxane (SCU-PR), in which scutellarin (SCU) was covalently bound to one of the hydroxyl groups of polyrotaxane (PR), was synthesized, and its characterization was further investigated by NMR, XRD, TG, DSC. The cytotoxicity of SCU-PR was assessed in vitro using human HCT116 and LOVO cell lines in results that the IC50 values of SCU-PR (1.03×10(-6) and 1.01×10(-6)mol/L, respectively), which compared with those of free SCU (7.80×10(-5) and 7.70×10(-5)mol/L, respectively), were lower. The valuable properties of SCU-PR will be potentially useful for its application on human colon cancer chemotherapies.

Keywords: Characterization; Cyclodextrin; Cytotoxicity; Polyrotaxane; Preparation; Scutellarin.

Publication types

  • Evaluation Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • Apigenin / chemistry*
  • Apigenin / pharmacology
  • Cell Line, Tumor
  • Cyclodextrins / chemistry*
  • Drug Carriers / chemistry*
  • Glucuronates / chemistry*
  • Glucuronates / pharmacology
  • Humans
  • Inhibitory Concentration 50
  • Poloxamer / chemistry*
  • Rotaxanes / chemistry*
  • Safety
  • Solubility
  • Temperature
  • Water / chemistry

Substances

  • Antineoplastic Agents
  • Cyclodextrins
  • Drug Carriers
  • Glucuronates
  • Rotaxanes
  • polyrotaxane
  • Water
  • Poloxamer
  • scutellarin
  • Apigenin