title: Design and synthesis of dual-ligand modified chitosan as a liver targeting vector.
abstract: Vector plays an important role in hepatic targeted drug delivery system. In this study, a novel material as a liver targeting vector, dual-ligand modified chitosan (GCGA) composed of chitosan (CTS), glycyrrhetinic acid (GA) and lactobionic acid (LA), was designed and synthesized by an orthogonal experiment with two-step synthesis under mild conditions. The synthesized final product was characterized and confirmed by FTIR and (1)H-NMR spectroscopy, and DS of GA and LA in CTS were measured to be 13.77 and 16.74 mol% using (1)H-NMR, respectively. The cytotoxicity of CTS and GCGA was concentration dependent which was inverse proportion to the cell viability by MTT assay using L929 cell line, and inhibitory concentration 50% (IC50) was 0.2 mg/ml for GCGA. The in vitro targeting efficiency and the in vitro cellular uptake were investigated. Compared with CTS NPs and GA-CTS NPs, GCGA NPs showed good cell specificity to BEL-7402 cells via the dual-ligand-receptor-mediated recognition, leading to a higher affinity to BEL-7402 cells. The results suggested that GCGA described here has the potential to be used as an effective vector for hepatic targeted drug therapy.
authors: Biomedical Materials and Engineering Center, Wuhan University of Technology, Wuhan, People's Republic of China.
authors: Houxiang
authors: H
authors: Chen
authors: Min
authors: M
authors: Li
authors: Tao
authors: T
authors: Wan
authors: Qichang
authors: Q
authors: Zheng
authors: Mingrong
authors: M
authors: Cheng
authors: Shiqi
authors: S
authors: Huang
authors: Yong
authors: Y
authors: Wang
mesh_terms: D000818:Animals; D045744:Cell Line, Tumor; D002470:Cell Survival; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D048271:Chitosan / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems; D015195:Drug Design; D005690:Galactose / Q000737:chemistry; D008401:Gas Chromatography-Mass Spectrometry / Q000379:methods; D006801:Humans; D008024:Ligands; D008099:Liver / Q000378:metabolism*; D009682:Magnetic Resonance Spectroscopy / Q000379:methods; D051379:Mice; D008956:Models, Chemical; D017550:Spectroscopy, Fourier Transform Infrared / Q000379:methods
chemical_list: D004337:Drug Carriers; D008024:Ligands; D048271:Chitosan; D005690:Galactose