RESUMEN
Polymers with targeted ligands are widely used as the anti-cancer drug delivery materials. For applications of chitosan as an anti-liver cancer drug delivery, poly (ethylene glycol)/lactobionic acid-grafted chitosan (PEG/LA-CS) was prepared and investigated since lactobionic acid can be specifically recognized by the hepatocytes. The structure of the PEG/LA-CS was characterized by Fourier transform infrared spectrometry and elemental analysis. The self-assembly behaviors of the PEG/LA-CS were monitored by steady-state fluorescence spectroscopy and electronic transmission microscope. The protein adsorption of the PEG/LA-CS was detected with bovine serum albumin (BSA) by electrochemical impedance spectroscopy. The results showed that the PEG/LA-CS almost did not adsorb protein. To study the effects of PEG/LA-CS on the structure of BSA, the interactions between the PEG/LA-CS and BSA were detected by ultraviolet spectrum, fluorescence spectrum, and circular dichroism. All the data gave one result that BSA maintained its original folded confirmation in PEG/LA-CS solution. The hemocompatibility of PEG/LA-CS was investigated by observing the effects of PEG/LA-CS on the hemolysis rate and the plasma recalcification time (PRT). The results showed that the PRT was prolonged greatly and the hemolysis rate was less than 5%. Furthermore, PEG/LA-CS also showed good cytocompatibility with K562, Hep G2, and LO2 cells. Therefore, the PEG/LA-CS is believed to have great potential for producing injectable anti-liver cancer drug delivery.
Asunto(s)
Materiales Biocompatibles/síntesis química , Materiales Biocompatibles/toxicidad , Quitosano/química , Disacáridos/química , Ensayo de Materiales , Polietilenglicoles/química , Adsorción , Animales , Materiales Biocompatibles/química , Coagulación Sanguínea/efectos de los fármacos , Bovinos , Línea Celular , Supervivencia Celular/efectos de los fármacos , Técnicas de Química Sintética , Hemólisis/efectos de los fármacos , Humanos , Albúmina Sérica Bovina/química , SolubilidadRESUMEN
Non-alcoholic steatohepatitis is a burgeoning health problem. To diagnose NASH with magnetic resonance imaging (MRI), an effective contrast agent, a stable suspension of superparamagnetic Fe(3)O(4) nanoparticles, were newly developed. The negatively charged Fe(3)O(4) nanoparticles were coated with positive chitosan (CS) firstly, and then assembled with poly(vinyl acetate-methylacrylic acid) (P(VAc-MAA)). Transmission electron microscope and dynamic light scattering confirmed that the obtained P(VAc-MAA)/CS/Fe(3)O(4) nanoparticles had a spherical or ellipsoidal morphology with an average diameter in the range of 14-20 nm. The superparamagnetic property and spinel structure of the Fe(3)O(4) nanoparticles were well preserved due to the protection of the P(VAc-MAA)/CS layers on the surface of the Fe(3)O(4) nanoparticles. The in vivo rat experiments confirmed that the P(VAc-MAA)/CS/Fe(3)O(4) nanoparticles were an effective contrast agent for MRI to diagnose NASH.
Asunto(s)
Acrilatos/química , Quitosano/química , Hígado Graso/metabolismo , Compuestos Férricos/química , Imagen por Resonancia Magnética/métodos , Nanopartículas/química , Compuestos de Vinilo/química , Animales , Medios de Contraste/farmacología , Luz , Magnetismo , Masculino , Microscopía Electrónica de Transmisión/métodos , Tamaño de la Partícula , Ratas , Ratas Sprague-Dawley , Dispersión de Radiación , Espectroscopía Infrarroja por Transformada de Fourier/métodos , Difracción de Rayos XRESUMEN
A novel simple method was developed to successfully synthesize biocompatible N-carboxyethylchitosan (NCECS) with a substitution degree of approx. 41% using the Michael addition reaction. The NCECS structure was characterized by Fourier transform infra-red spectrometry (FT-IR), (1)H-NMR, elemental analysis, X-ray diffraction spectrometry (XRD) and thermogravimetric analysis (TGA). The physicochemical properties of NCECS in solution are found to be strongly dependent on the pH value. In the pH range of 5.0-5.5, NCECS aggregates in dilute aqueous solution as evident by steady-state fluorescence spectroscopy and viscosimetry. The aggregated NCECS shows a spheric morphology from the atomic force microscopy (AFM) study. The possible aggregation mechanism was discussed.