Improved efficacy of doxorubicin delivery by a novel dual-ligand-modified liposome in hepatocellular carcinoma
Improved efficacy of doxorubicin delivery by a novel dual-ligand-modified liposome in hepatocellular carcinoma
复制标题
新型双配体修饰脂质体提高了肝细胞癌中阿霉素递送的功效。
DOI：
10.1016/j.canlet.2020.06.017
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发表时间：
2020-10-01
期刊：
影响因子：
9.7
通讯作者：
Gao, Zhiqin
中科院分区：
文献类型：
--
作者：
Li, Xiaocheng;Diao, Wenbin;Gao, Zhiqin
脂质体已被广泛用作生物医学研究和临床应用中的药物载体，允许稳定治疗化合物并克服细胞和组织摄取的障碍。然而，脂质体的靶向效率仍然很低，导致对肿瘤细胞的杀伤不足，对正常细胞造成不必要的损伤。本研究以大黄酸（GA）和花生凝集素（PNA）为配体，制备双配体修饰阿霉素脂质体（DOX-GA/PNA-Lips），以提高其对肝癌的靶向性和疗效。PNA和GA修饰增强了脂质体与肝癌细胞的结合能力，导致DOXGA/PNA-Lips具有优异的组织和细胞靶向性。DOX-GA/PNA-Lips在体内和体外均显示出有效的抗肿瘤作用，其靶向递送有助于减轻DOX的毒副作用。这些结果表明，双配体修饰的脂质体可能为肝癌的治疗提供一种有效的策略。
Liposomes have been widely used as drug carriers in both biomedical research and for clinical applications, allowing the stabilisation of therapeutic compounds and overcoming obstacles to cellular and tissue uptake. However, liposomes still have low targeting efficiency, resulting in insufficient killing of tumour cells and unnecessary damage to normal cells. In this study, glycyrrhetinic acid (GA) and peanut agglutinin (PNA) were used as ligands to prepare dual-ligand-modified doxorubicin-loaded liposomes (DOX-GA/PNA-Lips) to enhance the targeting accuracy and efficacy of drug delivery against malignant liver cancer. PNA and GA modification enhanced the binding ability of liposomes to liver cancer cells, leading to excellent tissue and cell targeting of DOXGA/PNA-Lips. DOX-GA/PNA-Lips showed an effective anti-tumour effect in vivo and in vitro, with its targeted delivery facilitating attenuation of the toxic side effects of DOX. These results demonstrated that dual-ligand-modified liposomes may provide an effective strategy for the treatment of hepatocellular carcinoma.