Biodistribution properties of nanoparticles based on mixtures of PLGA with PLGA-PEG diblock copolymers

The basic characteristics and the biodistribution properties of nanoparticles prepared from mixtures of poly(lactide-co-glycolide) (PLGA) with poly(lactide-co-glycolide)-poly(ethylene glycol) (PLGA-PEG) copolymers were investigated. A PLGA(45)-PEG(5) copolymer of relatively low PEG content and a PLGA(5)-PEG(5) copolymer of relatively high PEG content were included in the study. Increasing the PLGA-PEG content of the PLGA/PLGA-PEG mixture, or when PLGA(45)-PEG(5) was replaced by PLGA(5)-PEG(5), a decrease in the size of the nanoparticles and an increase in the rate of PEG loss from the nanoparticles were observed. The blood residence of the PLGA/PLGA(45)-PEG(5) nanoparticles increased as their PLGA-PEG content was increased, reaching maximum blood longevity at 100% PLGA(45)-PEG(5). On the contrary, the blood residence of PLGA/PLGA(5)-PEG(5) nanoparticles exhibited a plateau maximum in the range of 80-100% PLGA(5)-PEG(5). At PLGA-PEG proportions lower than 80%, the PLGA/PLGA(45)-PEG(5) nanoparticles exhibited lower blood residence than the PLGA/PLGA(5)-PEG(5) nanoparticles, whereas at PLGA-PEG proportions higher than 80%, the PLGA/PLGA(45)-PEG(5) nanoparticles exhibited higher blood residence than the PLGA/PLGA(5)-PEG(5) nanoparticles. These findings indicate that apart from the surface PEG content, the biodistribution properties of the PLGA/PLGA-PEG nanoparticles are also influenced by the size of the nanoparticles and the rate of PEG loss from the nanoparticles. (c) 2005 Elsevier B.V. All rights reserved.