Effect of copolymer composition on the physicochemical characteristics, in vitro stability, and biodistribution of PLGA-mPEG nanoparticles.
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.
Avgoustakis
K
K
Pharmaceutical Technology Laboratory, Department of Pharmacy, University of Patras, Rion 26500, Patras, Greece. avgoust@upatras.gr
Beletsi
A
A
Panagi
Z
Z
Klepetsanis
P
P
Livaniou
E
E
Evangelatos
G
G
Ithakissios
D S
DS
D000818:Animals; D002122:Calcium Chloride / Q000737:chemistry; D002850:Chromatography, Gel; D003102:Colloids; D003692:Delayed-Action Preparations; D005260:Female; D007275:Injections, Intravenous; D019344:Lactic Acid / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics*; D009682:Magnetic Resonance Spectroscopy; D008657:Metabolic Clearance Rate; D051379:Mice; D008970:Molecular Weight; D036103:Nanotechnology; D010316:Particle Size; D011092:Polyethylene Glycols / Q000737:chemistry* / Q000493:pharmacokinetics*; D011100:Polyglycolic Acid / Q000737:chemistry* / Q000493:pharmacokinetics*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers / Q000737:chemistry* / Q000493:pharmacokinetics*; D011877:Radionuclide Imaging; D013431:Sulfates / Q000737:chemistry; D013499:Surface Properties; D014018:Tissue Distribution
D003102:Colloids; D003692:Delayed-Action Preparations; D011108:Polymers; D013431:Sulfates; C012036:sodium sulfate; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011092:Polyethylene Glycols; C028210:monomethoxypolyethylene glycol; D002122:Calcium Chloride