负载雷公藤红素的中空介孔聚多巴胺纳米复合物的制备及体外抗肿瘤活性研究

Preparation of celastrol-loaded hollow mesoporous polydopamine nanocomposite and its in vitro antitumor activity

目的 制备负载雷公藤红素的中空介孔聚多巴胺纳米复合物(H-PDA/Cel@HA),并考察其体外抗肿瘤活性研究。方法 采用湿化学刻蚀法制备H-PDA/Cel@HA,通过粒径、Zeta电位、透射电镜、紫外吸收光谱等方法对其进行表征,并从细胞毒性、细胞活性氧水平测定、活/死细胞染色实验、细胞凋亡等方面评价H-PDA/Cel@HA对乳腺癌4T1细胞的抗肿瘤活性。结果 所制备的H-PDA/Cel@HA呈现出中空立方体的形貌,平均粒径为(183.4±12.3)nm,Zeta电位为(-30.4±1.1)mV;载药量为(13.25±1.16)%,包封率为(66.27±5.78)%;H-PDA/Cel@HA显著抑制乳腺癌4T1细胞的生长,相较于游离的Cel,其对正常细胞(L929)具有更好的生物相容性。此外,H-PDA/Cel@HA还通过增加4T1细胞内的活性氧水平,诱导细胞凋亡。结论 所制备的H-PDA/Cel@HA具有良好的生物相容性和肿瘤靶向递送能力,可有效抑制肿瘤细胞的生长。

Objective To prepare hollow mesoporous polydopamine nanocomposites loaded with celastrol(H-PDA/Cel@HA)and investigate in vitro antitumor activity.Methods The were synthesized via a wet chemical etching method.The nanocomposites were characterized using techniques such as particle size analysis,Zeta potential measurement,transmission electron microscopy,and ultraviolet absorption spectroscopy.The antitumor activity of H-PDA/Cel@HA against breast cancer 4T1 cells was assessed through cytotoxicity assays,evaluation of cellular reactive oxygen species(ROS)levels,live/dead cell staining experiments,and apoptosis analysis.Results The H-PDA/Cel@HA exhibited a hollow cubic morphology,with an average particle size of(183.4±12.3)nm.The Zeta potential values of H-PDA/Cel@HA was(-30.4±1.1)mV.The drug loading rate was(13.25±1.16)%,with an encapsulation rate of(66.27±5.78)%.H-PDA/Cel@HA demonstrated significant inhibition of breast cancer 4T1 cell growth and exhibits better biocompatibility with normal cells(L929)compared to free Cel.Moreover,H-PDA/Cel@HA increased the ROS levels in 4T1 cells and induced apoptosis.Conclusion H-PDA/Cel@HA exhibit promising biocompatibility,exhibit promising biocompatibility,tumor-targeted delivery ability,and can effectively inhibit the growth of tumor cells,and can effectively inhibit the growth of tumor cells.