中文摘要：

利用寡聚乙二醇（ mOEG）修饰海藻酸钠（ ALG）,有效降低了ALG的黏度,提高了其对疏水性肝靶向配体甘草次酸（ GA）的负载量.结果表明,靶向材料（ GA-ALG-mOEG）的 GA负载量为11.8%,是对照组（ GA-ALG）的1.97倍.在此基础上,以物理交联的方式引入pH响应的阿霉素前药（ DOX-ALG-mOEG）,制备了肝靶向纳米前药（ DOX-ALG-mOEG/GA-ALG-mOEG NPs）.细胞实验及抑瘤实验结果表明,该前药较对照组（ DOX-ALG/GA-ALG NPs）具有更高的肝靶向性和药物利用率,其对肝癌细胞的半致死率浓度（ IC50）为58.1 ng/mL,是对照组（ IC50=141.7 ng/mL）的41%；动物实验结果显示,该前药的抑瘤率达到了88.4%,比对照组提高了11.5%.

英文摘要：

The high viscosity of sodium alginate（ ALG） causes its insufficient targeted ligand loading, and further influences the targeted recognition effect of nano-prodrug. Here, oligomeric ethylene glycol modified-sodium alginate（ ALG-mOEG） was used as a carrier to improve the targeted-ligands loading. Results showed that ALG-mOEG significantly improved glycyrrhetinic acid （ GA ） loading compared with unmodified ALG （11.8% vs. 6.9%, 1.97-fold increase） . On this basis, the liver targeted nano-prodrug（ DOX-ALG-mOEG/GA-ALG-mOEG NPs ） was self-assembled via dialysis method by mixing GA-ALG-mOEG and DOX-ALG-mOEG. Cell cytotoxicity experiment showed that DOX-ALG-mOEG/GA-ALG-mOEG NPs inhibited HepG2 proliferation with an half maximal inhibitory concentration（ IC50 ） value of 58.1 ng/mL while the IC50 of control group was 141.7 ng/mL;the tumor growth inhibition rate（ IR） reached to 88.4%, improved by 11.5% com-pared to that of the control group. This study show that the liver targeted nano-prodrug based on ALG-mOEG can effectively improve the drug utilization, and provide a reference for the preparation of other polysaccharide targeted nano-prodrug.