Key Laboratory of Functional Polymer Materials, Ministry of Education, Institute of Polymer Chemistry, Nankai University, Tianjin, P. R. China.
Nanomedicine. 2012 Aug;8(6):870-9. doi: 10.1016/j.nano.2011.11.002. Epub 2011 Nov 16.
A drug carrier based on glycyrrhetinic acid-modified sulfated chitosan (GA-SCTS) was synthesized. The glycyrrhetinic acid (GA) acted as both a hydrophobic group and a liver-targeting ligand. The GA-SCTS micelles displayed rapid and significant ability to target the liver in vivo. The IC(50) for doxorubicin (DOX)-loaded GA-SCTS micelles (DOX/SA-SCTS micelles) against HepG2 cells was 54.7 ng/mL, which was extremely lower than the amount of no-GA-modified DOX-loaded micelles. In addition, DOX/SA-SCTS micelles could target specifically the liver cancer cells. They had higher affinity for the liver cancer cells (HepG2 cells) than for the normal liver cells (Chang liver cells). There was nearly 2.18-fold improvement in uptake of the DOX/SA-SCTS micelles by HepG2 cells than that by Chang liver cells. These results indicate that GA-SCTS is not only an excellent carrier for drugs, but also a potential vehicle for liver-cancer targeting.
基于甘草次酸修饰的硫酸化壳聚糖（GA-SCTS）的药物载体被合成。甘草次酸（GA）既作为疏水性基团又作为肝靶向配体。GA-SCTS 胶束在体内具有快速和显著的靶向肝脏的能力。载多柔比星（DOX）的 GA-SCTS 胶束（DOX/SA-SCTS 胶束）对 HepG2 细胞的 IC50 为 54.7ng/mL，远低于无 GA 修饰的载 DOX 胶束的量。此外，DOX/SA-SCTS 胶束可以特异性地靶向肝癌细胞。它们对肝癌细胞（HepG2 细胞）的亲和力高于正常肝细胞（Chang 细胞）。HepG2 细胞对 DOX/SA-SCTS 胶束的摄取率比 Chang 细胞高近 2.18 倍。这些结果表明，GA-SCTS 不仅是一种优秀的药物载体，也是一种潜在的肝癌靶向载体。
