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聚(乳酸-羟基乙酸)-聚乙二醇-修饰的人参皂苷 Rg3 纳米药物增强肝癌的抗肿瘤作用。

Poly(lactic acid hydroxyacetic acid)-poly(ethylene glycol)-modified ginsenoside Rg3 nanomedicine enhances anti-tumor effect in hepatocellular carcinoma.

机构信息

Department of Oncology, The Second Affiliated Hospital of Anhui Medical University, Hefei, China.

Institute of Translational Medicine, Zhejiang University, Hangzhou, China.

出版信息

Drug Dev Ind Pharm. 2024 Aug;50(8):763-775. doi: 10.1080/03639045.2024.2402769. Epub 2024 Sep 16.

Abstract

OBJECTIVE

This research aims to improve the bioavailability and anti-hepatocellular carcinoma (HCC) efficacy of Ginsenoside Rg3 by modification with poly (lactic acid hydroxyacetic acid)-poly(ethylene glycol) (PLGA-PEG).

METHODS

PLGA-PEG-Rg3 was obtained by emulsification and evaluated it physiochemical characterization by FTIR, SEM, laser particle-size analyzer and HPLC. The effect of the PLGA-PEG-Rg3 and Rg3 on HepG2 cells was compared studies, including cell proliferation, transwell and a series of apoptosis detection, and HCC model.

RESULTS

The PLGA-PEG-Rg3 were 122 nm in size and 0.112 in polydispersity index with sustained release profile . Compared to Rg3, PLGA-PEG-Rg3 was more effective in suppressing HepG2 growth and inducing apoptosis by the mitochondrial apoptosis pathway . And PLGA-PEG modification enhanced the liver-targeting ability and drug circulation time of Rg3 , resulting in PLGA-PEG-Rg3 possessing superior performance in inhibiting tumor growth and prolonging the survival time of tumor-bearing mice than Rg3.

CONCLUSIONS

Overall, these results showed PLGA-PEG-Rg3 enhanced the anti-tumor effect of Rg3 in HCC.

摘要

目的

本研究旨在通过聚(乳酸羟基乙酸)-聚(乙二醇)(PLGA-PEG)修饰来提高人参皂苷 Rg3 的生物利用度和抗肝癌(HCC)疗效。

方法

通过乳化法得到 PLGA-PEG-Rg3,并通过傅里叶变换红外光谱(FTIR)、扫描电子显微镜(SEM)、激光粒度分析仪和高效液相色谱(HPLC)对其理化性质进行评价。通过细胞增殖、Transwell 实验和一系列凋亡检测以及 HCC 模型比较了 PLGA-PEG-Rg3 和 Rg3 对 HepG2 细胞的影响。

结果

PLGA-PEG-Rg3 的粒径为 122nm,多分散指数为 0.112,具有持续释放的特点。与 Rg3 相比,PLGA-PEG-Rg3 更能有效抑制 HepG2 生长,并通过线粒体凋亡途径诱导细胞凋亡。PLGA-PEG 修饰增强了 Rg3 的肝靶向能力和药物循环时间,使得 PLGA-PEG-Rg3 在抑制肿瘤生长和延长荷瘤小鼠生存时间方面优于 Rg3。

结论

综上所述,这些结果表明 PLGA-PEG-Rg3 增强了 Rg3 在 HCC 中的抗肿瘤作用。

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