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引用本文:孙晶晶,席建军,童巧,曹宇,邵益丹,潘旭旺,张璐,史婷婷,何若愚,庄让笑.半乳糖胺修饰聚酰胺-胺树状大分子包载黄芩苷纳米复合物的制备及抗肝癌作用研究[J].中国现代应用药学,2026,43(10):68-77.
sunjingjing,xijianjun,tongqiao,caoyu,shaoyidan,panxuwang,zhanglu,shitingting,heruoyu,zhuangrangxiao.The preparation and anti-liver cancer effect of galactosamine-modified polyamide-amine dendrimers loaded with baicalin nanocomposites[J].Chin J Mod Appl Pharm(中国现代应用药学),2026,43(10):68-77.
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半乳糖胺修饰聚酰胺-胺树状大分子包载黄芩苷纳米复合物的制备及抗肝癌作用研究
孙晶晶, 席建军, 童巧, 曹宇, 邵益丹, 潘旭旺, 张璐, 史婷婷, 何若愚, 庄让笑
杭州市西溪医院
摘要:
目的:制备新型肝靶向黄芩苷/PAMAM-Gal纳米复合物,并对其进行质量评价及体外抗肝癌细胞活性研究。方法:采用傅里叶红外光谱(FT-IR)和核磁共振氢谱(1H NMR)确证PAMAM-Gal载体的结构,并对黄芩苷/PAMAM-Gal纳米复合物的粒径、电位、载药量、包封率、体外释放特性及肝癌细胞抑制活性进行研究。结果:成功制备黄芩苷/PAMAM-Gal纳米复合物,其粒径为(386.4±10.0) nm,zeta电位为(-5.3±1.79) mV,载药量为(16.9±4.8)%,包封率为(19.6±3.4)%,体外释药特性符合缓释制剂特征,可显著抑制肝癌细胞MHCC97H的活力,并能够阻滞细胞周期至G0/G1期。结论:本实验获得了较为理想的新型肝靶向黄芩苷/PAMAM-Gal纳米复合物,对肝癌细胞活性具有优异的抑制作用,能够阻碍MHCC97H肝癌细胞周期进程。
关键词:  黄芩苷  聚酰胺-胺型树枝状高分子  半乳糖胺  体外释放  抗癌活性
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The preparation and anti-liver cancer effect of galactosamine-modified polyamide-amine dendrimers loaded with baicalin nanocomposites
sunjingjing, xijianjun, tongqiao, caoyu, shaoyidan, panxuwang, zhanglu, shitingting, heruoyu, zhuangrangxiao
Affiliated hangzhou Xixi Hospital, Zhejiang Chinese Medical University ,Hangzhou Zhejiang
Abstract:
ABSTRACT:OBJECTIVE This study aimed to prepare a novel liver-targeting nanocomposite (Baicalin/PAMAM-Gal) and evaluate its inhibitory effects against hepatocellular carcinoma (HCC) cells. METHODS The PAMAM-Gal carrier was characterized using the ourier transform infrared spectroscopy and the transmission electron microscopy. The particle size distribution and zeta potential of Baicalin/PAMAM-Gal nanoparticles were determined using a laser particle size analyzer.HPLC was applied to evaluate the drug loading, encapsulation efficiency and in vitro release rate. The cytotoxicity of the nanoparticles against HCC cells was evaluated via CCK-8 assay. RESULTS The nanoparticles exhibited an average diameter of 386.4 ± 10.0 nm and a zeta potential of -5.3 ± 1.79 mV. The drug loading and encapsulation efficiency were (16.85±4.82) % and (19.6%±3.4) %. In vitro release studies demonstrated sustained drug release from the nanocomposite. Notably, Baicalin/PAMAM-Gal nanoparticles significantly inhibited the viability of MHCC97H liver cancer cells and was able to block the cell cycle at G0/G1. CONCLUSION This study successfully developed an optimized liver-targeting Baicalin/PAMAM-Gal nanocomposite with potent anti-HCC activity and could hinder cycle progression of MHCC97H cells, suggesting its potential as a promising therapeutic candidate.
Key words:  Baicalin  Polyamide-amine dendrimer  Galactosamine  in vitro release  anticancer activity
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