二氢杨梅素纳米粒的制备及其体外抗肿瘤研究

Preparation and in vitro anti-tumor evaluation of dihydromyricetin-loaded nanoparticles

目的制备并表征二氢杨梅素聚乙二醇-聚乳酸羟基乙酸纳米粒(DMY NPs)。方法采用乳化溶剂挥发法制备DMY NPs,透射电镜观察纳米粒的外观形态;纳米粒度分析仪分析其粒径大小及分布;高效液相色谱法测定其包封率及载药量;考察其稳定性和体外释药特性;MTT法和Annexin V/PI双染法分别考察纳米粒对人膀胱癌EJ细胞的抑制及促凋亡作用。结果制备的DMY NPs平均粒径为214 nm,TEM结果显示纳米粒呈圆整球形或类球形,且分布均匀,包封率为83.36%,载药量为4.04%。DMY NPs具有良好的稳定性和缓释能力。体外细胞实验结果显示,DMY NPs能有效地抑制人膀胱癌EJ细胞的增殖并诱导细胞凋亡。结论构建的二氢杨梅素纳米粒具有良好的缓释特性,能有效增强药物的体外抗肿瘤活性。

Objective To prepare and characterize the dihydromyricetin-loaded methoxy polyethylene glycol-polylactic acid glycolic acid nanoparticles(DMY NPs).Methods DMY NPs were prepared by emulsification-solvent evaporation method.The morphology imaging was determined by transmission electron microscopy.The particle size was measured by a nanoparticle analyzer.The drug-loading rate and encapsulation efficiency were determined by HPLC.The stability and drug release characteristics in vitro were determined.The cytotoxicity was determined by MTT and cell apoptosis by flow cytometry.Results The optimal DMY NPs were around 214 nm in size.The TEM showed uniform spherical morphology.The encapsulation efficiency and drug loading of DMY NPs were 83.36%and 4.04%,respectively.In addition,the nanoparticles exhibited good stability and sustained release feature.MTT and flow cytometry indicated that DMY NPs enhanced the cytotoxicity and increased the apoptotic level in the EJ cells effectively.Conclusion DMY NPs display good drug sustained-release capacity in vitro,and significantly enhance the antitumor activity.