Doxorubicin-conjugated PLA-PEG-Folate based polymeric micelle for tumor-targeted delivery: synthesis and in vitro evaluation

Daru. 2014 Mar 6;22(1):30. doi: 10.1186/2008-2231-22-30.

Abstract

Background: Selective delivery of anticancer agents to target areas in the body is desirable to minimize the side effects while maximizing the therapeutic efficacy. Anthracycline antibiotics such as doxorubicin (DOX) are widely used for treatment of a wide variety of solid tumors.This study evaluated the potential of a polymeric micellar formulation of doxorubicin as a nanocarrier system for targeted therapy of a folate-receptor positive human ovarian cancer cell in line.

Results: DOX-conjugated targeting and non-targeting micelles prepared by the dialysis method were about 188 and 182 nm in diameter, respectively and their critical micelle concentration was 9.55 μg/ml. The DOX-conjugated micelles exhibited a potent cytotoxicity against SKOV3 human ovarian cancer cells. Moreover, the targeting micelles showed higher cytotoxicity than that of non-targeting ones (IC₅₀= 4.65 μg/ml vs 13.51 μg/ml).

Conclusion: The prepared micelle is expected to increase the efficacy of DOX against cancer cells and reduce its side effects.

MeSH terms

  • Antineoplastic Agents / administration & dosage*
  • Antineoplastic Agents / therapeutic use
  • Cell Line, Tumor
  • Doxorubicin / administration & dosage*
  • Doxorubicin / therapeutic use
  • Drug Carriers / administration & dosage*
  • Drug Carriers / chemistry
  • Drug Delivery Systems
  • Female
  • Folic Acid / chemistry
  • Humans
  • Micelles
  • Ovarian Neoplasms / drug therapy*
  • Ovarian Neoplasms / pathology
  • Particle Size
  • Polyethylene Glycols / chemical synthesis
  • Tetrazolium Salts / pharmacology
  • Thiazoles / pharmacology

Substances

  • Antineoplastic Agents
  • Drug Carriers
  • Micelles
  • Tetrazolium Salts
  • Thiazoles
  • monomethoxypolyethyleneglycol-polylactide block copolymer
  • Polyethylene Glycols
  • Doxorubicin
  • Folic Acid
  • thiazolyl blue