Preparation and evaluation of vinblastine PCL-PEG-PCL nanoparticles / 中国药科大学学报

ABSTRACT

Aim:To prepare vinblastine-loaded PCL-PEG_(6000)-PCL nanoparticles,and to study their physicochemi-cal properties and in vitro antitumor activity.Methods: PCL-PEG_(6000)-PCL triblock copolymer was prepared by ring-opening polymerization,and vinblastine-loaded PCL-PEG_(6000)-PCL nanoparticles was prepared by coprecipita-tion.The morphous,particle size,polydisperse index,particle yield,the drag-loading content,the encapsulation ef-ficiency and in vitro release rate of these vinblastine-loaded nanoparticles were determined.The cytotoxicity of vinblastine-loaded nanoparticles to K562/A02 leukimia cell line was determined by MTT assay.Results: It was found using transmission electron microscopy(TEM)that the nanoparticles exhibited a spherical shape with core-shell structure.The particle sizes of the nanoparticles obtained by dynamic light scattering were(185 ± 2.7)nm.The drug loading content and the encapsulation efficiency were determined to be 28.83% and 86.52%,re-spectively.In vitro release study revealed that more than 70% of accumulative release of entrapped vinblastine was reached in 9 hr and that nearly complete release was achieved in 24 hr.The inhibition of vinblastine-loaded nanoparticles to K562/A02 cell line was significantly increased as compared with that of the same dose of sulfate vinblastine solution.Conclusions: PCL-PEG-PCL nanoparticles could be used as a carrier of vinblastine,and the prepared nanoparticles exhibited a spherical shape,high encapsulation efficiency,relevant stablity and sustained-release properties.The eytotoxicity of vinblastine to K562/A02 cell line was significantly increased when it was encapsulated in PCL-PEG-PCL nanoparticles.