Preparation, characterization and antioxidation activity in vitro of quercetin loaded chitosan nanoparticles / 中国生化药物杂志

ABSTRACT

Objective To prepare quercetin ( QUE) loaded chitosan nanoparticles ( CS-NPs), evaluate its physicochemical properties and antioxidation activity in vitro.Methods Quercetin chitosan nanoparticles were prepared by ionic crosslinking method and self-assembly method.The preparation method was optimized using entrapment efficiency (EE), drug loading (DL) and size as indexes.The best formulation and preparation conditions were optimized by orthogonal test based on single-factor test, evaluation indicator as particle size and EE.The physicochemical properties of the obtained QUE-CS-NPs were characterized by the following methods: the transmission electron microscope (TEM), dynamic light scattering (DLS) analysis for morphology, size distribution and Zeta potential.In vitro release behavior in 0.5% SDS solution was evaluated by dialysis tube method.In vitro antioxidant activity assays were performed by evaluating the abilities of the microspheres for hydroxide radicals and superoxide anions .Results TEM results revealed QUE-CS-NPs with round and uniform.Particle-size analysis showed that the diameters and Zeta potential of the QUE-CS-NPs were (282.9 ±20) nm and (30.5 ±2) mV, with uniform distribution (polydispersity below 0.185).DL and EE of QUE-CS-NPs were (8.81 ±0.65) %and (80.02 ±1.04) %, respectively.QUE-CS-NPs showed extended administration times with 66.2% cumulative release within 72 h.QUE-CS-NPs showed pronounced antioxidant activity and a concentration dependent, even more substantial than that of pure QUE.Conclusion QUE-CS-NPs show a good size, sustain release effect and pronounce antioxidant activity.