Time- and concentration-dependent apoptosis and necrosis induced by free and HPMA copolymer-bound doxorubicin in human ovarian carcinoma cells

J Control Release. 2000 Oct 3;69(1):185-96. doi: 10.1016/s0168-3659(00)00301-1.

Abstract

A2780 sensitive and A2780/AD doxorubicin (DOX) resistant human ovarian carcinoma cells were exposed to different concentrations (0.25, 0.5, 1, 5 and 10xIC(50)) of free and HPMA copolymer-bound DOX for 12, 24, 36, 48, 60 and 72 h. Apoptosis and necrosis were evaluated using the FITC-conjugated annexin V and propidium iodide staining. The data obtained showed that the induction of apoptosis and necrosis by both free DOX and HPMA copolymer-bound DOX were time- and concentration-dependent. The data also showed significant differences between the drugs. It was found that: (i) under the action of HPMA copolymer-bound doxorubicin the alterations in the plasma membrane permeability preceded disturbances in cellular metabolism; (ii) HPMA copolymer-bound doxorubicin kills the cells mainly by necrosis; (iii) HPMA copolymer-bound doxorubicin is a more effective anticancer drug than free doxorubicin.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adult
  • Antibiotics, Antineoplastic / administration & dosage*
  • Antibiotics, Antineoplastic / pharmacology*
  • Apoptosis / drug effects*
  • Cell Membrane / drug effects
  • Cell Membrane / ultrastructure
  • Cell Membrane Permeability / drug effects
  • Doxorubicin / administration & dosage*
  • Doxorubicin / pharmacology*
  • Female
  • Genes, MDR / genetics
  • Humans
  • Methacrylates / chemistry*
  • Mitochondria / metabolism
  • Necrosis
  • Ovarian Neoplasms / drug therapy*
  • Ovarian Neoplasms / pathology*
  • Phosphatidylserines / chemistry
  • Time Factors
  • Tumor Cells, Cultured

Substances

  • Antibiotics, Antineoplastic
  • Methacrylates
  • Phosphatidylserines
  • Doxorubicin
  • hydroxypropyl methacrylate