Cai Yuee, Xu Yingqi, Chan Hon Fai, Fang Xiaobin, He Chengwei, Chen Meiwan
State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau , Macau 999078, China.
Department of Biomedical Engineering, Columbia University , New York 10027, United States.
Mol Pharm. 2016 Mar 7;13(3):699-709. doi: 10.1021/acs.molpharmaceut.5b00677. Epub 2016 Jan 25.
Glycyrrhetinic acid (GA), the main hydrolysate of glycyrrhizic acid extracted from the root of licorice, has been used in hepatocellular carcinoma (HCC) therapy. Particularly, GA as a ligand in HCC therapy has been widely explored in different drug delivery systems, including liposomes, micelles, and nanoparticles. There is considerable interest worldwide with respect to the development of GA-modified drug delivery systems due to the extensive presence of GA receptors on the surface of hepatocyte. Up until now, much work has been focused on developing GA-modified drug delivery systems which bear good liver- or hepatocyte-targeted efficiency both in vitro and in vivo. Owing to its contribution in overcoming the limitations of low lipophilicity and poor bioavailability as well as its ability to promote receptor-mediated endocytosis, GA-modified drug delivery systems play an important role in enhancing liver-targeting efficacy and thus are focused on the treatment of HCC. Moreover, since GA-modified delivery systems present more favorable pharmacokinetic properties and hepatocyte-targeting effects, they may be a promising formulation for GA in the treatment of HCC. In this review, we will give an overview of GA-modified novel drug delivery systems, paying attention to their efficacy in treating HCC and discussing their mechanism and the treatment effects.
甘草次酸（GA）是从甘草根部提取的甘草酸的主要水解产物，已用于肝细胞癌（HCC）治疗。特别是，GA作为HCC治疗中的一种配体，已在不同的药物递送系统中得到广泛研究，包括脂质体、胶束和纳米颗粒。由于肝细胞表面广泛存在GA受体，全球对GA修饰的药物递送系统的开发有着浓厚的兴趣。到目前为止，许多工作都集中在开发在体外和体内均具有良好的肝脏或肝细胞靶向效率的GA修饰药物递送系统。由于GA在克服低亲脂性和低生物利用度的局限性方面的贡献以及其促进受体介导的内吞作用的能力，GA修饰的药物递送系统在提高肝脏靶向疗效方面发挥着重要作用，因此专注于HCC的治疗。此外，由于GA修饰的递送系统具有更有利的药代动力学性质和肝细胞靶向作用，它们可能是GA治疗HCC的一种有前景的制剂。在这篇综述中，我们将概述GA修饰的新型药物递送系统，关注它们在治疗HCC方面的疗效，并讨论其作用机制和治疗效果。
