A cancer-recognizing polymeric photosensitizer based on the tumor extracellular pH response of conjugated polymers for targeted cancer photodynamic therapy

Macromol Biosci. 2014 Dec;14(12):1688-95. doi: 10.1002/mabi.201400361. Epub 2014 Sep 24.

Abstract

Herein, a cancer-recognizing polymeric photosensitizer (CRPP) was demonstrated not only for high water solubility but also for pH-responsive targeted photodynamic cancer therapy. The synthesized CRPP exhibited high water solubility and the pH-dependent charge-switching property. From an in vitro cellular internalization study with HCT-116 human colon cancer cells, significantly enhanced cellular uptake as detected for CRPP at pH 6.5 compared to the cellular uptake of CRPP at pH 7.4, which led to enhanced cytotoxicity in the cancer cells. Finally, the CRPP was found to exhibit high tumor-targeting efficacy in an in vivo tumor model and was finally excreted through the renal route.

Keywords: cancer; drug delivery; pH-responsive polymer; photodynamic therapy; photosensitizer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antineoplastic Agents* / chemistry
  • Antineoplastic Agents* / pharmacokinetics
  • Antineoplastic Agents* / pharmacology
  • Cell Line, Tumor
  • Colonic Neoplasms* / drug therapy
  • Colonic Neoplasms* / metabolism
  • Colonic Neoplasms* / pathology
  • Drug Delivery Systems / methods*
  • Humans
  • Hydrogen-Ion Concentration
  • Mice
  • Mice, Inbred BALB C
  • Mice, Nude
  • Photochemotherapy / methods*
  • Xenograft Model Antitumor Assays / methods

Substances

  • Antineoplastic Agents