Journal of Materials Science: Materials in Medicine 2011-04-01

Glycyrrhetinic acid-functionalized degradable micelles as liver-targeted drug carrier.

Wei Huang, Wei Wang, Ping Wang, Chuang-Nian Zhang, Qin Tian, Yue Zhang, Xiu-Hua Wang, Rui-Tao Cha, Chun-Hong Wang, Zhi Yuan

Index: J. Mater. Sci. Mater. Med. 22(4) , 853-63, (2011)

Full Text: HTML

Abstract

Recently, many efforts have been devoted to investigating the application of functionalized micelles as targeted drug delivery carriers. In this study, glycyrrhetinic acid (GA, a liver targeting ligand) modified poly(ethylene glycol)-b-poly(γ-benzyl L-glutamate) micelles were prepared and evaluated as a potential liver-targeted drug carrier. The aggregation behavior, stability, size and morphology of the micelles were investigated. Anticancer drug doxorubicin (DOX) was encapsulated in the micelles. The drug release profile, in vivo distribution and the cytotoxicity against hepatic carcinoma QGY-7703 cells of DOX-loaded micelles were studied. The results indicated that the release profile was pH-dependent with Fickian diffusion kinetics. The micelles were remarkably targeted to the liver, inducing a 4.9-fold higher DOX concentration than that for free DOX · HCl. The DOX-loaded micelles exhibited almost twofold more potent cytotoxicity compared with DOX · HCl, and the cytotoxicity was time- and dosage-dependent. These results suggest that GA-functionalized micelles represent a promising carrier for drug delivery to the liver.