目的 制备共载姜黄素和IR780的聚乳酸-羟基乙酸共聚物(poly lactic-co-glycolic acid，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/cm²、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 ζ potential 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/cm², 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.

R283.6

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