Abstract

The aim of our study was to investigate the blood clearance characteristics and biodistribution of polysaccharide surface-decorated PLA nanoparticles. For this purpose, cholesterol-modified dextran was synthesized and used as emulsion stabilizer for preparation of PLA nanoparticles by an o/w emulsion-evaporation technique. The influence of substituted degree (SD) of cholesterol on dextran chains and concentration of dextran–cholesterol on the size of PLA nanoparticles were studied via TEM and DLS. It was found that the optimal conditions were SD = 5% and C DEX–CH = 0.5 mg/ml to prepare dextran–cholesterol-coated PLA nanoparticles (DEX–CH/PLA) with the size about 105 nm and a narrow size distribution. The coating of polysaccharide on the surface of PLA nanoparticles was demonstrated by ζ-potential measurement, and the existence of polysaccharide remarkably reduced non-specific protein absorption. These polysaccharide-decorated PLA nanoparticles were injected intravenously into S–D rats and their blood clearance and biodistribution in vivo was studied using scintillation counter. The results showed that although the polysaccharide coating inhibits BSA absorption, but does not help in prolonging the blood circulation time compared with PVA stabilized PLA nanoparticles. The DEX–CH/PLA nanoparticles were captured mainly by liver, spleen, and lungs within 5 h after injection, while they were barely found in brain.

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