Department of Oncology, The Second Affiliated Hospital of Anhui Medical University, Hefei, China.
Institute of Translational Medicine, Zhejiang University, Hangzhou, China.
Drug Dev Ind Pharm. 2024 Aug;50(8):763-775. doi: 10.1080/03639045.2024.2402769. Epub 2024 Sep 16.
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).
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.
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.
Overall, these results showed PLGA-PEG-Rg3 enhanced the anti-tumor effect of Rg3 in HCC.
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。
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。
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。
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。
