PREPARATION AND CHARACTERIZATION OF GLYCYRRHETINIC ACID-MODIFIED POLOXAMER 188/CHITOSAN NANOPARTICLES

In this paper, we firstly synthesized glycyrrhetinic acid-modified double amino-terminated poloxamer 188 (GA–NH–POLO–NH–GA). The structure of the synthesized compound was confirmed by ¹H-NMR and Fourier transform infrared (FT-IR) spectroscopy. Then the nanoparticles composed of GA–NH–POLO–NH–GA/chitosan (GA–NH–POLO–NH–GA/CTS) were prepared by an ionic gelation process. The characterization of the nanoparticles was measured by dynamic light scattering (DLS) and scanning electron microscope (SEM). The results showed that the nanoparticles were well dispersed with a spherical shape and the particle size was distributed between 100 nm and 300 nm. The cytotoxicity based on MTT assay against cells (QGY-7703 cells and L929 cells) showed that the nanoparticles had low toxicity and good biocompatibility. The encapsulation efficiency and drug loading of 5-fluorouracil-loaded nanoparticles (5-FU nanoparticles) were measured by high-performance liquid chromatography (HPLC) and fluorescence spectroscopy, ultraviolet-visible (UV-vis) absorbance. The encapsulation of 5-Fu-loaded CTS nanoparticles was 12.8% and the drug loading was 2.9%, while the encapsulation of 5-Fu-loaded GA–NH–POLO–NH–GA/CTS nanoparticles was 20.9% and the drug loading was 3.36%. The release profile showed that the GA–NH–POLO–NH–GA/CTS nanoparticles were available for sustained release of 5-Fu. The GA–NH–POLO–NH–GA/CTS nanoparticles have a higher affinity to the QGY-7703 cells, so indicated that the GA–NH–POLO–NH–GA/CTS nanoparticles have the capacity of liver-targeting in vitro.