Delivering a hydrophobic anticancer drug for photodynamic therapy by amorphous formulation

Bioorg Med Chem Lett. 2010 Nov 1;20(21):6172-4. doi: 10.1016/j.bmcl.2010.08.132. Epub 2010 Sep 16.

Abstract

An amorphous formulation of hypocrellin A for photodynamic therapy is reported which can provide stable aqueous dispersion of such hydrophobic photosensitizers. In vitro studies have demonstrated the active uptake of amorphous formulation of hypocrellin A into the mitochondria of tumor cells. Compared with Tween-80 micelle embedded hypocrellin A, low dark-toxicity but similar light-toxicity of the amorphous one to drug impregnated tumor cells was observed. Thus, the potential of using amorphous formulation of hypocrellin A as drug delivery system for photodynamic therapy has been demonstrated.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Benzimidazoles
  • Cell Death
  • Chemistry, Pharmaceutical
  • Coloring Agents
  • DNA, Mitochondrial / drug effects
  • Dose-Response Relationship, Drug
  • Drug Delivery Systems
  • Fluorescent Dyes
  • HeLa Cells
  • Humans
  • Micelles
  • Mitochondria / metabolism
  • Perylene / administration & dosage
  • Perylene / analogs & derivatives*
  • Perylene / chemistry
  • Perylene / isolation & purification
  • Phenol
  • Photochemotherapy*
  • Photosensitizing Agents / administration & dosage*
  • Photosensitizing Agents / chemistry*
  • Photosensitizing Agents / isolation & purification
  • Polysorbates
  • Quinones / administration & dosage*
  • Quinones / chemistry*
  • Quinones / isolation & purification
  • Spectrometry, Fluorescence
  • Surface-Active Agents
  • Tetrazolium Salts
  • Thiazoles
  • X-Ray Diffraction

Substances

  • Benzimidazoles
  • Coloring Agents
  • DNA, Mitochondrial
  • Fluorescent Dyes
  • Micelles
  • Photosensitizing Agents
  • Polysorbates
  • Quinones
  • Surface-Active Agents
  • Tetrazolium Salts
  • Thiazoles
  • Phenol
  • Perylene
  • thiazolyl blue
  • bisbenzimide ethoxide trihydrochloride
  • hypocrellin A