熊果酸
树枝状大分子
化学
体内
生物利用度
两亲性
结合
细胞毒性
生物化学
药理学
癌症研究
体外
生物
有机化学
聚合物
色谱法
生物技术
共聚物
数学分析
数学
作者
Zhichun Shen,Bowen Li,Yajun Liu,Guirong Zheng,Yan Guo,Rui Zhao,Kai Jiang,Lulu Fan,Jingwei Shao
标识
DOI:10.1016/j.nano.2017.10.007
摘要
Ursolic acid (UA), a natural triterpene acid, is a promising anti-cancer drug due to its inhibitory effect on tumor growth and metastasis. However, clinical translation of UA is limited by its poor water solubility and low bioavailability. To overcome these problems, herein an amphiphilic self-assembly nanodrug composed of UA, lactobionic acid (LA) and low-polyamidoamine (low-PAMAM) dendrimers is developed. This near-spherical nanodrug with a uniform size (~180 nm) demonstrated to have an enhanced cytotoxicity against liver cancer SMMC7721 cells, and could attenuate the migration and adhesion of SMMC7721 cells at non-toxic concentrations by suppressing metastasis-related protein MMP-9 expression. Furthermore, in vivo study indicates that the nanodrug exhibited prolonged circulation time in blood as well as increased AUC, MRT and Cmax, and could effectively inhibit the tumor growth in H22 mice model. Overall, the UA-based nanodrug delivery system reported in the present work represents a novel strategy for targeted tumor therapy.
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