Institute of Medicine and Drug Research, Qiqihar Medical University, Qiqihar, PR China.
Carbohydr Polym. 2021 Apr 1;257:117572. doi: 10.1016/j.carbpol.2020.117572. Epub 2021 Jan 5.
Hyaluronic acid (HA)-coated liposomes were designed for the targeted delivery of 17-hydroxy-jolkinolide B (HA-Lip-HJB). HA-Lip-HJB had a particle size of 130.8 ± 1.9 nm, zeta potential of -52.36 ± 1.91 mV, and encapsulation efficiency of 89.2 ± 1.5 %. In vitro cell experiments indicated that modification of HA-Lip-HJB increased its cytotoxicity and cellular uptake via CD44 receptor-mediated endocytosis pathway. Of particular importance is that HA-Lip-HJB suppressed cell migration and invasion by inhibiting epithelial-mesenchymal transition (EMT) process. Moreover, the HA-Lip-HJB displayed notable growth inhibition on tumor spheroids. Furthermore, in vivo tissue distribution and anti-tumor experiments carried on BALB/C mice bearing 4T1 tumor indicated that HA-Lip-HJB had strong tumor targeting and tumor suppression abilities. The results also demonstrated that HA-Lip-HJB inhibited tumor cells migration and colonization on the lung. Therefore, HA-Lip-HJB is a promising formulation for metastatic breast cancer therapy.
透明质酸(HA)包覆脂质体被设计用于 17-羟基-乔利金内酯 B(HA-Lip-HJB)的靶向递送。HA-Lip-HJB 的粒径为 130.8±1.9nm,Zeta 电位为-52.36±1.91mV,包封率为 89.2±1.5%。体外细胞实验表明,通过 CD44 受体介导的内吞途径修饰 HA-Lip-HJB 增加了其细胞毒性和细胞摄取。特别重要的是,HA-Lip-HJB 通过抑制上皮-间充质转化(EMT)过程抑制细胞迁移和侵袭。此外,HA-Lip-HJB 对肿瘤球体显示出明显的生长抑制作用。此外,在携带 4T1 肿瘤的 BALB/C 小鼠上进行的体内组织分布和抗肿瘤实验表明,HA-Lip-HJB 具有很强的肿瘤靶向和肿瘤抑制能力。结果还表明,HA-Lip-HJB 抑制了肿瘤细胞在肺部的迁移和定植。因此,HA-Lip-HJB 是一种有前途的转移性乳腺癌治疗制剂。