Fluorine-18 labeled galactosylated chitosan for asialoglycoprotein-receptor-mediated hepatocyte imaging

Yang, Wenjiang; Mou, Tiantian; Guo, Wenyan; Jing, Huihui; Peng, Cheng; Zhang, Xianzhong; Ma, Yonggang; Liu, Boli

doi:10.1016/j.bmcl.2010.06.106

Cited by 27 publications

(11 citation statements)

References 13 publications

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“…As reported in the literature, HepG2 cells were found with overexpressed ASGPR on the cell surfaces and A549 cells were not found to express ASGPR (Yang et al, 2010). The cells were incubated in DMEM medium supplemented with 10% FBS and 1% ciprofloxacin solution at 37 C, 5% CO 2 .…”

Section: Cytotoxic Viability Assaymentioning

confidence: 91%

In vitro and in vivo evaluation of macromolecular prodrug GC-FUA based nanoparticle for hepatocellular carcinoma chemotherapy

Huang

Gao

et al. 2017

Drug Delivery

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A novel type of macromolecular prodrug delivery system is reported in this research. The N-galactosylated-chitosan-5-fluorouracil acetic acid conjugate (GC-FUA) based nanoparticle delivery system was evaluated in vitro and in vivo. Biocompatibility of GC-FUA-NPs was screened by BSA adsorption test and hemolysis activity examination in vitro. Cytotoxicity and cellular uptake study in HepG2 and A549 cells demonstrated that compared to free 5-Fu, the GC-FUA-NPs play great function in killing cancer cells for the cell endocytosis mediated by asialoglycoprotein receptor (ASGPR), which overexpresses on the cell surface. Pharmacokinetics study further illustrated that the drug-loaded nanoparticles has a much longer half-time than free 5-Fu in blood circulation in Sprague-Dawley (SD) rats. Tissue distribution was investigated in Kunming mice, and the result showed that the GC-FUA-NPs have a long circulation effect. The obtained data suggested that GC-FUA-NP is a very promising drug delivery system for efficient treatment of hepatocellular carcinoma.

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Section: Cytotoxic Viability Assaymentioning

confidence: 91%

In vitro and in vivo evaluation of macromolecular prodrug GC-FUA based nanoparticle for hepatocellular carcinoma chemotherapy

Huang

Gao

et al. 2017

Drug Delivery

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“…Moreover, other problems exist, such as sensitivity to changes of temperature and pH and the introduction of toxic byproducts during synthesis. Recently, radiotracers using chitosan or dextran as the backbone were developed (4,(17)(18)(19). Those tracers showed specific and rapid targeting of hepatocytes.…”

Section: Discussionmentioning

confidence: 99%

“…Galactosylated dextran or chitosan were able to bind to hepatocytes because of the galactose residue positioned on the exterior of the polymer (16). Radiotracers using dextran or chitosan as the backbone, such as 99m Tc-labeled Cy5.5-DTPA-galactosyl-dextran (17), 99m Tc-galactosyl-methylated chitosan (18), 99m Tc-hydrazinonicotinamide-galactosylated chitosan (4), and 18 F-fluorobenzoate-galactosylated chitosan (19), have been developed.…”

mentioning

confidence: 99%

Copolymer-Based Hepatocyte Asialoglycoprotein Receptor Targeting Agent for SPECT

Yang

Mou²,

Shao³

et al. 2011

J Nucl Med

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Poly(vinylbenzyl-O-b-D-galactopyranosyl-D-gluconamide) (PVLA) can be specifically internalized by hepatocytes via the asialoglycoprotein receptor. In this study, we synthesized and characterized galactose-carrying copolymers with hydrazinonicotinamide chains as bifunctional groups to radiolabel PVLA with 99m Tc for SPECT targeting specific hepatocytes. Methods:The copolymer was labeled with 99m Tc using tricine as a coligand. Then 99m Tc[P(VLA-co-VNI)](tricine) 2 was evaluated by in vivo metabolic stability and biodistribution in normal mice. SPECT was performed in normal New Zealand White rabbits and rabbits with liver cancer. Results: 99m Tc[P(VLA-co-VNI)](tricine) 2 was prepared in high labeling yield (.95%) and radiochemical purity (.99%), with good stability. The results of biodistribution in mice demonstrated that the liver uptake was 125.33 6 10.99 percentage injected dose per gram at 10 min after injection and could be blocked significantly by preinjecting free neogalactosylalbumin or P(VLA-co-VNI). SPECT images with high quality were obtained at 15, 30, 60, and 120 min after injection of the radiotracer. Significant radioactivity defect was observed in the liver cancer model. Conclusion: The bifunctional coupling agent hydrazinonicotinamide was introduced to PVLA via copolymerization and labeled with 99m Tc. The promising biologic properties of 99m Tc[P(VLA-co-VNI)](tricine) 2 afford potential applications for the assessment of hepatocyte function in the future.

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“…Currently, studies about drug delivery systems mainly focus on single-targeted drug delivery systems, 6,7 such as the chitosan (CTS)-based drug delivery system, which allows liver-targeting drug delivery using specific interactions between galactose and the asialoglycoprotein receptor (ASGP-R) expressed on liver or hepatoma cells surface. 8 Another ligand used in liver-targeting drug delivery is glycyrrhetinic acid (GA), which is enriched in liver tissues.…”

Section: Cheng Et Almentioning

confidence: 99%

Synthesis of liver-targeting dual-ligand modified GCGA/5-FU nanoparticles and their characteristics in vitro and in vivo

Cheng¹,

Gao²,

Wang³

et al. 2013

IJN

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Nanoparticle drug delivery systems using polymers hold promise for clinical applications. We synthesized dual-ligand modified chitosan (GCGA) nanoparticles using lactic acid, glycyrrhetinic acid, and chitosan to target the liver in our previous studies. We then synthesized the GCGA/5-FU nanoparticles by conjugating 5-fluorouracil (5-FU) onto the GCGA nanomaterial, which had a mean particle size of 239.9 nm, a polydispersity index of 0.040, a zeta potential of +21.2 mV, and a drug loading of 3.90%. GCGA/5-FU nanoparticles had good slow release properties, and the release process could be divided into five phases: small burst release, gentle release, second burst release, steady release, and slow release. Inhibitory effects of GCGA/5-FU on tumor cells targeted the liver, and were time and dose dependent. GCGA nanoparticles significantly prolonged the efficacy of 5-FU on tumor cells, and alleviated the resistance of tumor cells to 5-FU. GCGA/5-FU nanoparticles were mostly concentrated in the liver, indicating that the GCGA nanoparticles were liver targeting. GCGA/5-FU nanoparticles significantly suppressed tumor growth in orthotopic liver transplantation mouse model, and improved mouse survival.

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Fluorine-18 labeled galactosylated chitosan for asialoglycoprotein-receptor-mediated hepatocyte imaging

Cited by 27 publications

References 13 publications

In vitro and in vivo evaluation of macromolecular prodrug GC-FUA based nanoparticle for hepatocellular carcinoma chemotherapy

In vitro and in vivo evaluation of macromolecular prodrug GC-FUA based nanoparticle for hepatocellular carcinoma chemotherapy

Copolymer-Based Hepatocyte Asialoglycoprotein Receptor Targeting Agent for SPECT

Synthesis of liver-targeting dual-ligand modified GCGA/5-FU nanoparticles and their characteristics in vitro and in vivo

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