School of Bioscience and Technology, Shandong Key Lab of Medical and Health Sciences, Key Lab of Biotechnological Medicine in Universities of Shandong, Weifang Medical University, Weifang, 261053, China.
Weifang Second People's Hospital, 7 Yuanxiao Street, Weifang, 261041, China.
Cancer Lett. 2020 Oct 1;489:163-173. doi: 10.1016/j.canlet.2020.06.017. Epub 2020 Jun 25.
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 DOX-GA/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.
脂质体已被广泛应用于生物医学研究和临床应用中，作为药物载体，以稳定治疗化合物，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较低，导致肿瘤细胞的杀伤不足，对正常细胞造成不必要的损伤。在本研究中，甘草次酸（GA）和花生凝集素（PNA）被用作配体，制备了载多柔比星的双配体修饰脂质体（DOX-GA/PNA-Lips），以提高针对恶性肝癌的药物输送的靶向准确性和疗效。PNA 和 GA 修饰增强了脂质体与肝癌细胞的结合能力，使 DOX-GA/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 的毒性副作用。这些结果表明，双配体修饰的脂质体可能为治疗肝细胞癌提供一种有效的策略。
