Experimental Study Of Sodium Ozagrel Long-Circulating Nanoparticles Modified By PEG And Its Pharmacokinetics In Animal

Objectives: The biodegradable macromolecular poly(ethylene glycol)-poly (D,L-lac- tide) block copolymer (PEG-PLA) was synthesized by opening ring polymerization, then long-circulating nanoparticles containing sodium ozagrel (SOG-LCN), which can release in a long time, was prepared by modern nanoparticles preparation technique, in which PEG-PLA was used as carrier and SOG was used as model drug. SOG-LCN could lengthened the drug's biological half-life largely because SOG-LCN could keep away from phagotrophy from the mononuclear phagocytic system(MPS), and it also could improve stability of SOG. Uniform experimental design methods coupled with computerized optimization was adopted to screen the formulation and preparation process. The surface morphology, average diameter and size distribution for long-circulating nanoparticles were studied by various methods. To establish the quality control standard for SOG-LCN, the encapsulation efficiency, drug loading content and release in vitro were also examined by various experiments. At last, pharmacokinetics in rabbits was investigated to evaluate its effect of sustained-release in vivo. Through the discussing of mechanisms how long-circulating nanoparticles could release in a long time, we expect to provide scientific theoretical basis for SCRDDS about nanoparticles preparation.Methods: Poly(ethylene glycol)-poly(D,L-lactide) block copolymer (PEG-PLA) was synthesized by opening ring polymerization from D,L-lactide and PEG6000, and viscosity-average molecular weight for PEG-PLA was determined...