Pectin nanoparticle enhances cytotoxicity of methotrexate against HepG2 cells

Drug Deliv. 2013;20(1):1-9. doi: 10.3109/10717544.2012.739214. Epub 2012 Dec 8.

Abstract

Objective: This work has aimed to develop methotrexate-conjugated pectin nanoparticle for delivering a cytotoxic drug to hepatic cancer cell.

Methods: Methotrexate was conjugated to pectin by carbodiimide chemistry. Nanoparticles of pectin conjugated with methotrexate (MTX) were then fabricated by using ionotropic gelation. The size, shape and surface charge were characterized by dynamic light scattering and microscopic method. Cytotoxicity of MTX-pectin nanoparticle was monitored by MTT assay.

Results: Methotrexate-pectin nanoparticle was successfully formulated. Drug release study indicated that MTX-NP exhibited sustained drug release at pH 7.4. Sustained release of methotrexate may enable methotrexate-pectin nanoparticle as a controlled drug delivery system. Cytotoxicity study confirmed the activity of the drug incorporated in nanoparticles. In addition, the cytotoxicity of methotrexate was increased when conjugated to pectin nanoparticles, compared to free methotrexate.

Conclusions: This study verified that pectin can deliver methotrexate to hepatic cancer cell and provide sustained drug delivery. The cytotoxicity of methotrexate was enhanced when methotrexate was conjugated to pectin indicating the improved drug delivery to cancer cell.

MeSH terms

  • Antimetabolites, Antineoplastic / administration & dosage
  • Antimetabolites, Antineoplastic / chemistry*
  • Cytotoxins / administration & dosage
  • Cytotoxins / chemistry*
  • Drug Delivery Systems / methods*
  • Hep G2 Cells
  • Humans
  • Methotrexate / administration & dosage
  • Methotrexate / chemistry*
  • Nanoparticles / administration & dosage
  • Nanoparticles / chemistry*
  • Pectins / administration & dosage
  • Pectins / chemistry*

Substances

  • Antimetabolites, Antineoplastic
  • Cytotoxins
  • Pectins
  • Methotrexate