Self-assembled nanoparticles based on galactosylated O-carboxymethyl chitosan-graft-stearic acid conjugates for delivery of doxorubicin

Int J Pharm. 2013 Dec 15;458(1):31-8. doi: 10.1016/j.ijpharm.2013.10.020. Epub 2013 Oct 17.

Abstract

A novel polymer, i.e. galactosylated O-carboxymethyl chitosan-graft-stearic acid (Gal-OCMC-g-SA) was synthesized for liver targeting delivery of doxorubicin. The chemical structure was characterized by FT-IR, (1)H NMR and elemental analysis. Gal-OCMC-g-SA could self-assemble into nanoparticles with diameter of 160 nm by probe sonication in aqueous medium and exhibited a low critical aggregation concentration of 0.047 mg/mL. The DOX-loaded Gal-OCMC-g-SA (Gal-OCMC-g-SA/DOX) self-assembled nanoparticles were almost spherical in shape with an average diameter of less than 200 nm and zeta potential of around -10 mV. In vitro release revealed that the Gal-OCMC-g-SA/DOX nanoparticles exhibited a sustained and pH-dependent drug release manner. Furthermore, the hemolysis test demonstrated the good safety of Gal-OCMC-g-SA in blood-contacting applications. These results indicated that Gal-OCMC-g-SA/DOX nanoparticles were highly potential to be applied in cancer therapy.

Keywords: Doxorubicin; Liver targeting; O-carboxymethyl chitosan; Stearic acid.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Chitosan / administration & dosage
  • Chitosan / analogs & derivatives*
  • Chitosan / chemistry
  • Doxorubicin / administration & dosage
  • Doxorubicin / chemistry*
  • Drug Carriers / administration & dosage
  • Drug Carriers / chemistry
  • Drug Delivery Systems / methods
  • Liver / metabolism
  • Nanoparticles / administration & dosage
  • Nanoparticles / chemistry*
  • Particle Size
  • Polymers / administration & dosage
  • Polymers / chemistry
  • Stearic Acids / administration & dosage
  • Stearic Acids / chemistry*

Substances

  • Drug Carriers
  • O-carboxymethylchitosan
  • Polymers
  • Stearic Acids
  • stearic acid
  • Doxorubicin
  • Chitosan