Zhang Xue, Lin Cong-Cong, Chan Wai-Kei-Nickie, Liu Kang-Lun, Yang Zhi-Jun, Zhang Hong-Qi
School of Chinese Medicine, Hong Kong Baptist University, Hong Kong, China.
Changshu Research Institute, Hong Kong Baptist University, Changshu Economic and Technological Development (CETD) Zone, Changshu 215500, China.
Molecules. 2017 Jun 24;22(7):1052. doi: 10.3390/molecules22071052.
PEGylated liposomes have received much attention as pharmaceutical carriers to deliver chemotherapeutic agents for therapeutic purpose. The aim of this study was to prepare and characterize PEGylated liposome of cantharidin and investigate its therapeutic effect on human hepatocellular carcinoma treatment in vitro and in vivo. Liposomal cantharidin was evaluated for their anticancer effects in vitro using human hepatocellular carcinoma HepG2 cells and in vivo using HepG2-bearing nude mice compared to free drug. PEGylated liposome of cantharidin had a particle size of 129.9 nm and a high encapsulation efficacy of approximately 88.9%. The liposomal cantharidin had a higher anti-proliferative effect vis-à-vis free cantharidin in inducing G2/M cell cycle arrest and apoptosis. Liposomal cantharidin killed more HepG2 cancer cells at the same concentration equivalent to free cantharidin. Further study in vivo also showed that liposomal cantharidin achieved a higher tumor growth inhibition efficacy than free drug on hepatocellular carcinoma. As our study exhibited enhanced cytotoxicity against HepG2 cells and augmented tumor inhibitory effects in vivo, the results validate the potential value of cantharidin-liposome in improving the therapeutic efficacy of cantharidin for liver cancer.
聚乙二醇化脂质体作为用于递送化疗药物以达到治疗目的的药物载体已受到广泛关注。本研究的目的是制备并表征斑蝥素的聚乙二醇化脂质体，并研究其在体外和体内对人肝癌治疗的效果。与游离药物相比，使用人肝癌HepG2细胞在体外评估脂质体斑蝥素的抗癌效果，并使用荷HepG2裸鼠在体内评估其抗癌效果。斑蝥素聚乙二醇化脂质体的粒径为129.9 nm，包封率约为88.9%，较高。脂质体斑蝥素在诱导G2/M期细胞周期阻滞和凋亡方面比游离斑蝥素具有更高的抗增殖作用。在相同浓度下，脂质体斑蝥素比游离斑蝥素杀死更多的HepG2癌细胞。体内进一步研究还表明，脂质体斑蝥素对肝癌的肿瘤生长抑制效果比游离药物更高。由于我们的研究显示对HepG2细胞具有增强的细胞毒性，并在体内增强了肿瘤抑制作用，结果证实了斑蝥素脂质体在提高斑蝥素对肝癌治疗效果方面的潜在价值。
