高等学校化学学报Issue(8)：1835-1842,8.DOI:10.7503/cjcu20131236
基于海藻酸钠衍生物的肝靶向纳米前药的构建及抗肿瘤活性研究
Preparation of Liver-targeted Nano-prodrug Based on Sodium Alginate Derivative and the Study on Antitumor Activity
摘要
Abstract
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.关键词
海藻酸钠衍生物/寡聚乙二醇/甘草次酸/抗肿瘤活性Key words
Sodium alginate derivative/Ethylene glycol oligomer/Glycyrrhetinic acid/Antitumor activity分类
化学化工引用本文复制引用
郭华,杨承玲,王蔚,赖全勇,袁直..基于海藻酸钠衍生物的肝靶向纳米前药的构建及抗肿瘤活性研究[J].高等学校化学学报,2014,(8):1835-1842,8.基金项目
国家自然科学基金(批准号:51073080,51273095)、天津市自然科学基金(批准号:13JCYBJC25100)和教育部创新团队PCSIRT 项目(批准号:IRT1257)资助.Supported by the National Natural Science Foundation of China(Nos.51073080,51273095), the Natural Science Foundation of Tianjin, China(No.13JCYBJC25100) and the Program for Changjiang Scholars and Innovative Research Team in University, China(No. IRT1257) （批准号:51073080,51273095）
