Docetaxel-loaded polylactic acid-co-glycolic acid nanoparticles: formulation, physicochemical characterization and cytotoxicity studies

J Nanosci Nanotechnol. 2013 Aug;13(8):5948-56. doi: 10.1166/jnn.2013.7735.

Abstract

In the present study, we developed novel docetaxel (DTX)-loaded polylactic acid-co-glycolic acid (PLGA) nanoparticles (NPs) using the combination of sodium lauryl sulfate (SLS) and poloxamer 407, the anionic and non-ionic surfactants respectively for stabilization. The NPs were prepared by emulsification/solvent evaporation method. The combination of these surfactants at weight ratio of 1:0.5 was able to produce uniformly distributed small sized NPs and demonstrated the better stability of NP dispersion with high encapsulation efficiency (85.9 +/- 0.6%). The drug/polymer ratio and phase ratio were 2:10 and 1:10, respectively. The optimized formulation of DTX-loaded PLGA NPs had a particle size and polydispersity index of 104.2 +/- 1.5 nm and 0.152 +/- 0.006, respectively, which was further supported by TEM image. In vitro release study was carried out with dialysis membrane and showed 32% drug release in 192 h. When in vitro release data were fitted to Korsmeyer-Peppas model, the n value was 0.481, which suggested the drug was released by anomalous or non-Fickian diffusion. In addition, DTX-loaded PLGA NPs in 72 h, displayed approximately 75% cell viability reduction at 10 microg/ml DTX concentration, in MCF-7 cell lines, indicating sustained release from NPs. Therefore, our results demonstrated that incorporation of DTX into PLGA NPs could provide a novel effective nanocarrier for the treatment of cancer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / administration & dosage
  • Cell Line, Tumor
  • Docetaxel
  • Dose-Response Relationship, Drug
  • Drug Carriers
  • Drug Delivery Systems
  • Humans
  • Ions / chemistry
  • Lactic Acid / chemistry*
  • Microscopy, Electron, Transmission
  • Models, Statistical
  • Nanoparticles / chemistry*
  • Nanotechnology / methods*
  • Particle Size
  • Poloxamer / administration & dosage
  • Poloxamer / chemistry
  • Polyglycolic Acid / chemistry*
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polymers / chemistry
  • Sodium Dodecyl Sulfate / chemistry
  • Surface Properties
  • Surface-Active Agents / chemistry
  • Taxoids / administration & dosage*
  • Time Factors

Substances

  • Antineoplastic Agents
  • Drug Carriers
  • Ions
  • Polymers
  • Surface-Active Agents
  • Taxoids
  • Poloxamer
  • Docetaxel
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyglycolic Acid
  • Lactic Acid
  • Sodium Dodecyl Sulfate