共载姜黄素和IR780的聚乳酸-羟基乙酸共聚物纳米粒的制备及其体外抗肿瘤评价  

Preparation and in vitro antitumor evaluation of PLGA nanoparticles co-loaded with curcumin and IR780

作　　者：黄华婷 吴念 蔡梦如 尹东阁 付婷婷 朱荣玥 尹兴斌[1] 梁潇 倪健[1] 董晓旭[1] HUANG Hua-ting;WU Nian;CAI Meng-ru;YIN Dong-ge;FU Ting-ting;ZHU Rong-yue;YIN Xing-bin;LIANG Xiao;NI Jian;DONG Xiao-xu(School of Chinese Material Medica,Beijing University of Chinese Medicine,Beijing 102488,China;Bionorica(Beijing)Technology Development Co.,Ltd.,Beijing 100020,China)

机构地区：[1]北京中医药大学中药学院,北京102488 [2]比奥罗历加(北京)科技发展有限公司,北京100020

出　　处：《中草药》2023年第2期498-508,共11页Chinese Traditional and Herbal Drugs

基　　金：中央高校基本科研业务费专项资金资助项目(2022-JYB-XJSJJ015)。

摘　　要：目的 制备共载姜黄素和IR780的聚乳酸-羟基乙酸共聚物(polylactic-co-glycolicacid,PLGA)纳米粒(curcumin/IR780 PLGA nanoparticles,Cur/IR780-NPs)并对其进行表征和体外抗肿瘤评价。方法 采用乳化溶剂挥发法制备Cur/IR780-NPs,用马尔文激光粒度仪、X射线粉末衍射仪、傅里叶变换红外光谱仪、紫外可见分光光度计、透射电子显微镜对其进行表征;HPLC和紫外可见分光光度计分别测定姜黄素和IR780载药量,并考察Cur/IR780-NPs稳定性和体外释药性能;利用人肝癌HepG2细胞模型考察Cur/IR780-NPs的细胞摄取和体外抗肿瘤效果。结果 Cur/IR780-NPs形态呈球形,平均粒径为(224.10±7.06)nm、多分散指数(polydispersity index,PDI)为0.081±0.013、ζ电位为(-9.84±0.16)mV,具有良好的稳定性。Cur/IR780-NPs能够有效负载姜黄素和IR780,载药量分别为(2.21±0.07)%、(2.35±0.31)%,具有近红外光谱响应性释药性能。Cur/IR780-NPs能够被HepG2细胞有效摄取,经808 nm激光(2.0 W/cm^(2)、5 min)照射后产生光热效应,与姜黄素发挥联合抗肿瘤作用。结论 Cur/IR780-NPs有助于将姜黄素和IR780共递送至HepG2细胞内,发挥化疗-光热治疗联合抗肿瘤作用,提高肝癌的治疗效果。Objective To prepare curcumin-IR780 nanoparticles(Cur/IR780-NPs) and investigate their characterization and antitumor activity in vitro. Methods Cur/IR780-NPs were prepared by emulsion solvent evaporation method, and characterized them by Malvern laser particle size analyzer, X-ray diffraction(XRD), Fourier transform infrared spectroscopy(FT-IR), UV-visible spectrophotometer, transmission electron microscopy(TEM). The drug loading of curcumin and IR780 were determined by HPLC and UV-visible spectrophotometer respectively, and the stability and release profiles of Cur/IR780-NPs were examined. The cellular uptake and cytotoxicity of Cur/IR780-NPs were evaluated on human liver cancer HepG2 cells. Results Cur/IR780-NPs displayed spherical shape and good stability, with a mean particle size of(224.10 ± 7.06) nm, polydispersity index(PDI) of 0.081 ± 0.013 and ζpotential of(-9.84 ± 0.16) mV. Cur/IR780-NPs could effectively load curcumin and IR780, and the drug loading was(2.21 ± 0.07)%and(2.35 ± 0.31)%, respectively. Cur/IR780-NPs could be effectively take up by HepG2 cells, and generated photothermal therapy after irradiation by 808 nm laser(2.0 W/cm^(2), 5 min), and combined with curcumin to improve anti-tumor efficiency. Conclusion Cur/IR780-NPs were helpful to deliver curcumin and IR780 into HepG2 cells and exerted the anti-tumor effect of chemo-photothermal therapy, which could improve the treatment efficiency of liver cancer.

关 键 词：姜黄素 IR780 纳米粒 PLGA 抗肿瘤 联合治疗 化疗-光热治疗 乳化溶剂挥发法 

分 类 号：R283.6[医药卫生—中药学]