Effect of copolymer composition on the physicochemical characteristics, in vitro stability, and biodistribution of PLGA-mPEG nanoparticles

Int J Pharm. 2003 Jun 18;259(1-2):115-27. doi: 10.1016/s0378-5173(03)00224-2.

Abstract

The physicochemical properties, the colloidal stability in vitro and the biodistribution properties in mice of different PLGA-mPEG nanoparticle compositions were investigated. The nanoparticles were prepared by a precipitation-solvent evaporation technique. The physical characteristics and the colloidal stability of the PLGA-mPEG nanoparticles were significantly influenced by the composition of the PLGA-mPEG copolymer used to prepare the nanoparticles. PLGA-mPEG nanoparticles prepared from copolymers having relatively high mPEG/PLGA ratios were smaller and less stable than those prepared from copolymers having relatively low mPEG/PLGA ratios. All PLGA-mPEG nanoparticle compositions exhibited prolonged residence in blood, compared to the conventional PLGA nanoparticles. The composition of the PLGA-mPEG copolymer affected significantly the blood residence time and the biodistribution of the PLGA-mPEG nanoparticles in liver, spleen and bones. The in vivo behavior of the different PLGA-mPEG nanoparticle compositions did not appear to correlate with their in vitro stability. Optimum mPEG/PLGA ratios appeared to exist leading to long blood circulation times of the PLGA-mPEG nanoparticles. This may be associated with the effects of the mPEG/PLGA ratio on the density of PEG on the surface of the nanoparticles and on the size of the nanoparticles.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Calcium Chloride / chemistry
  • Chromatography, Gel
  • Colloids
  • Delayed-Action Preparations
  • Female
  • Injections, Intravenous
  • Lactic Acid / blood
  • Lactic Acid / chemistry*
  • Lactic Acid / pharmacokinetics*
  • Magnetic Resonance Spectroscopy
  • Metabolic Clearance Rate
  • Mice
  • Molecular Weight
  • Nanotechnology
  • Particle Size
  • Polyethylene Glycols / chemistry*
  • Polyethylene Glycols / pharmacokinetics*
  • Polyglycolic Acid / chemistry*
  • Polyglycolic Acid / pharmacokinetics*
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polymers / chemistry*
  • Polymers / pharmacokinetics*
  • Radionuclide Imaging
  • Sulfates / chemistry
  • Surface Properties
  • Tissue Distribution

Substances

  • Colloids
  • Delayed-Action Preparations
  • Polymers
  • Sulfates
  • sodium sulfate
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyglycolic Acid
  • Lactic Acid
  • Polyethylene Glycols
  • monomethoxypolyethylene glycol
  • Calcium Chloride