Intracellular delivery of doxorubicin encapsulated in novel pH-responsive chitosan/heparin nanocapsules

Int J Nanomedicine. 2013:8:267-73. doi: 10.2147/IJN.S37737. Epub 2013 Jan 11.

Abstract

A novel polyelectrolyte nanocapsule system composed of biopolymers, chitosan and heparin has been fabricated by the layer-by-layer technique on silica nanoparticles followed by dissolution of the silica core. The nanocapsules were of the size range 200 ± 20 nm and loaded with the positively charged anticancer drug doxorubicin with an efficiency of 89%. The loading of the drug into the capsule happens by virtue of the pH-responsive property of the capsule wall, which is determined by the pKa of the polyelectrolytes. As the pH is varied, about 64% of the drug is released in acidic pH while 77% is released in neutral pH. The biocompatibility, efficiency of drug loading, and enhanced bioavailability of the capsule system was confirmed by MTT assay and in vivo biodistribution studies.

Keywords: biocompatible; drug delivery; electrostatic interaction; layer-by-layer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Chitosan / chemistry*
  • Doxorubicin / administration & dosage*
  • Doxorubicin / chemistry*
  • Doxorubicin / pharmacokinetics
  • Heparin / chemistry*
  • Humans
  • Hydrogen-Ion Concentration
  • Intracellular Space / metabolism*
  • MCF-7 Cells
  • Mice
  • Mice, Inbred BALB C
  • Nanocapsules / administration & dosage*
  • Nanocapsules / chemistry*
  • Static Electricity

Substances

  • Nanocapsules
  • Doxorubicin
  • Heparin
  • Chitosan