Macromolecular ligands with liver-targeting group (pyridoxamine, PM) PHEA-DTPA-PM and PAEA-DTPA-PM were prepared by the incorporation of different amount of diethylenetria-minepentaacetic acid monopyridoxamine group (...Macromolecular ligands with liver-targeting group (pyridoxamine, PM) PHEA-DTPA-PM and PAEA-DTPA-PM were prepared by the incorporation of different amount of diethylenetria-minepentaacetic acid monopyridoxamine group (DTPA-PM) into poly-α, β-[N-(2-hydroxyethyl)-L-aspartamide] (PHEA) and poly-α, β-[N-(2-aminoethyl)-L-aspartamide] (PAEA). The macromolecular ligands thus obtained were further complexed with gadolinium chloride to give macromolecular MRI contrast agents with different Gd(III) contents. These macromolecular ligands and their gadolinium complexes were characterized by1H NMR, IR, UV and elementary analysis. Relaxivity studies showed that these polyaspartamide gadolinium complexes possess higher relaxation effectiveness than that of the clinically used Gd-DTPA. Magnetic resonance imaging of the liver in rats and experimental data of biodistribution in mice indicate that these macromolecular MRI contrast agents containing pyridoxamine exhibit liver-targeting property.展开更多
Objective To prepare liver-targeted baicalin solid lipid nanoparticles(BSLNs) and to study their in vitro anti-oxidative activity.Methods BSLNs were prepared by emulsification ultrasonic dispersion method and characte...Objective To prepare liver-targeted baicalin solid lipid nanoparticles(BSLNs) and to study their in vitro anti-oxidative activity.Methods BSLNs were prepared by emulsification ultrasonic dispersion method and characterized by transmission electron microscopy and laser particle size distribution;The tissue in vivo distribution was detected by pharmacokinetics;In vitro anti-superoxide dismutase(SOD) activity and reduction capacity of BSLNs were determined;The ability of removing hydroxyl radical was determined by phenanthroline-Fe2+ oxidation.Results The best prescription was baicalin-soybean lecithin-glyceryl monostearate-poloxamer 188(1:5:15:30);The encapsulation efficiency and drug loading were 84.7% and 5.65%,respectively,mean size of particles was(68.6 ± 8) nm,Zeta potential was 22.13 mV;The in vitro anti-oxidant results showed that BSLNs had a significant inhibitory effect on SOD and a strong reducing capacity as well as a removing hydroxide radical ability.The targeting rate of BSLNs was 6.931 for liver.Conclusion The results demonstrate that BSLNs could enhance the liver targeting ability and in vitro anti-oxidative activity significantly.展开更多
基金Acknowledgements The authors would like to thank Mr. Cao Guoqiang and Mr. Cao Wei (Department of Nuclear Medicine of Wuhan Union Hospital) for their assistance in the biodistribution experiment, Profs. Zheng Congyi and Mr. Qu Sanfu (College of Life Scien
文摘Macromolecular ligands with liver-targeting group (pyridoxamine, PM) PHEA-DTPA-PM and PAEA-DTPA-PM were prepared by the incorporation of different amount of diethylenetria-minepentaacetic acid monopyridoxamine group (DTPA-PM) into poly-α, β-[N-(2-hydroxyethyl)-L-aspartamide] (PHEA) and poly-α, β-[N-(2-aminoethyl)-L-aspartamide] (PAEA). The macromolecular ligands thus obtained were further complexed with gadolinium chloride to give macromolecular MRI contrast agents with different Gd(III) contents. These macromolecular ligands and their gadolinium complexes were characterized by1H NMR, IR, UV and elementary analysis. Relaxivity studies showed that these polyaspartamide gadolinium complexes possess higher relaxation effectiveness than that of the clinically used Gd-DTPA. Magnetic resonance imaging of the liver in rats and experimental data of biodistribution in mice indicate that these macromolecular MRI contrast agents containing pyridoxamine exhibit liver-targeting property.
文摘Objective To prepare liver-targeted baicalin solid lipid nanoparticles(BSLNs) and to study their in vitro anti-oxidative activity.Methods BSLNs were prepared by emulsification ultrasonic dispersion method and characterized by transmission electron microscopy and laser particle size distribution;The tissue in vivo distribution was detected by pharmacokinetics;In vitro anti-superoxide dismutase(SOD) activity and reduction capacity of BSLNs were determined;The ability of removing hydroxyl radical was determined by phenanthroline-Fe2+ oxidation.Results The best prescription was baicalin-soybean lecithin-glyceryl monostearate-poloxamer 188(1:5:15:30);The encapsulation efficiency and drug loading were 84.7% and 5.65%,respectively,mean size of particles was(68.6 ± 8) nm,Zeta potential was 22.13 mV;The in vitro anti-oxidant results showed that BSLNs had a significant inhibitory effect on SOD and a strong reducing capacity as well as a removing hydroxide radical ability.The targeting rate of BSLNs was 6.931 for liver.Conclusion The results demonstrate that BSLNs could enhance the liver targeting ability and in vitro anti-oxidative activity significantly.
