Polymer carriers for anticancer drugs targeted to EGF receptor

Macromol Biosci. 2012 Dec;12(12):1714-20. doi: 10.1002/mabi.201200270. Epub 2012 Oct 17.

Abstract

A novel actively targeted polymer carrier for anticancer drugs based on an N-(2-hydroxypropyl)methacrylamide copolymer (PHPMA) is proposed. An oligopeptide sequence GE7, attached to the polymer, is a specific ligand for the EGF receptor overexpressed on most tumor cells. Co-attachment of selected chemotherapeutics will therefore lead to formation of tumor-specific polymer therapeutics, further enhanced by the EPR effect. FACS measurements prove elevated binding activity of the fluorescently labeled PHPMA/GE7 conjugate in EGFR-rich cells (FaDu, MCF-7), compared to conjugates of scrambled peptides. Cell lines with low EGFR level (SW620, B16F10) bind the GE7 conjugate significantly less.

Publication types

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

MeSH terms

  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / metabolism
  • Cell Line, Tumor
  • Chromatography, High Pressure Liquid
  • Drug Delivery Systems / methods*
  • ErbB Receptors / metabolism*
  • Flow Cytometry
  • Humans
  • Oligopeptides / genetics
  • Oligopeptides / metabolism
  • Polymethacrylic Acids / chemical synthesis
  • Polymethacrylic Acids / chemistry
  • Polymethacrylic Acids / therapeutic use*
  • Positron-Emission Tomography
  • Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization
  • Spectrophotometry, Ultraviolet

Substances

  • Antineoplastic Agents
  • Oligopeptides
  • Polymethacrylic Acids
  • Duxon
  • ErbB Receptors