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Preparation and Optimization of PEG-PLGA Loaded with Vincristine Sulfate and its In vitro Release

WEN Jia-Gen, GUO Tingting, ZHU Hong-Yuan, XIAO Yi-Yun, ZHANG Xiu-Zhen, CHEN Guo and CHEN Yuxiang

The aim of this study was to prepare the PEG-PLGA loaded with vincristine sulfate nanoparticles (VCR-loaded PEG-PLGA-NPs) and investigate its in vitro release properties. VCR-loaded PEG-PLGA-NPs were prepared by the modified double emulsion (W1/O/W2) method, and the main experimental factors influencing the characteristics of the nanoparticles were investigated and the preparation was optimized. The results showed that the physicochemical characteristics of VCR-loaded PEG-PLGA-NPs were affected by the polymer concentration, the ratio of internal water phase to oil phase, external water phase to oil phase and ultrasound time for the second time. VCR-loaded PEG-PLGA-NPs, with average particle size of 135.9nm, zeta potential of -12.83mV, encapsulation efficiency of 68.2% and drug loading of 8.34%, were prepared under optimal conditions. The release experiments in vitro showed the VCR release from PEG-PLGA-NPs exhibited consequently sustained release for more than 13d, which was in accordance with Higuchi equation.