Characterization and in-vitro bioactivity evaluation of paclitaxel-loaded polyester nanoparticles

Anticancer Drugs. 2012 Oct;23(9):947-58. doi: 10.1097/CAD.0b013e328355a6c6.

Abstract

Paclitaxel, an antimicrotubular agent used in the treatment of ovarian and breast cancer, was encapsulated in nanoparticles of poly(DL-lactide-co-glycolide) and poly(ε-caprolactone) polymers using the double emulsion-solvent evaporation technique. The morphology, size distribution, drug encapsulation efficiency, thermal degradation and in-vitro drug release profile were characterized. High-performance liquid chromatography was used to determine the drug encapsulation efficiency and in-vitro drug release profile. MCF-7 breast cancer cells were used to evaluate the cytotoxicity (MTT assay), the cellular uptake and the cell cycle. The particle size was in the range of 200-400 nm. Poly(lactide-co-glycolide) nanoparticles showed more effective cellular uptake compared with those of poly(ε-caprolactone). Unloaded nanoparticles were found to be cytocompatible on MCF-7 cells and paclitaxel formulations showed efficacy in killing MCF-7 cells. Paclitaxel-loaded nanoparticles induced the release of the drug-blocking cells in the G2/M phase. Paclitaxel-loaded nanoparticles may be considered a promising drug delivery system in the evaluation of an in-vivo model.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Culture Techniques
  • Cell Cycle / drug effects
  • Cell Survival / drug effects
  • Chromatography, High Pressure Liquid
  • Drug Carriers / chemistry*
  • Drug Compounding
  • Endocytosis / drug effects
  • Flow Cytometry
  • Humans
  • MCF-7 Cells
  • Microscopy, Fluorescence
  • Nanoparticles / chemistry*
  • Paclitaxel / administration & dosage
  • Paclitaxel / chemistry*
  • Paclitaxel / pharmacology*
  • Particle Size
  • Polyesters / chemistry*
  • Polyglactin 910 / chemistry*
  • Solubility
  • Surface Properties
  • Thermogravimetry

Substances

  • Drug Carriers
  • Polyesters
  • polycaprolactone
  • Polyglactin 910
  • Paclitaxel