Preparation and characterization of adriamycin-loaded chitosan nanoparticles surface-modified with glycyrrhizin

摘要

Aim To prepare and characterize the adriamycin-loaded chitosan nanoparticles surface-modified with glycyrrhizin (ADM-CS-NPs-GL) targeting to hepatocytes. Methods: adriamycin-loaded chitosan nanoparticles (ADM-CS-NPs)were prepared by ionic gelation method, and Glycyrrhizin (GL) was oxidized by sodium periodate to be conjugated to surface free amino groups of ADM-CS-NPs. Transmission electron microscopy was used to assess the shape of the nanoparticles. Malvern Zeta Nano-ZS was performed to measure the particlesize distribution. RP-HPLC was used to determine GL-binding ratio and ADM entrapment efficiency, as well as GL-binding stability and ADM release characteristic were investigated. Results: The ADM-CS-NPs-GL were spherical with an average diameter of 179.5 nm. The GL-binding ratio was 80% above and was still retained 65.2±3.4% after 12h in release medium. The ADM entrapment efficiency was 90% above. In vitro 28%±4.6%of ADM was slowly released from ADMCS -NPs-GL over a period of 72h, furthermore in the drug release process there was no drug "burst release". Conclusion: ADMCS -NPs-GL prepared with the simple method developed in this paper has properties of high drug entrapment efficient and high GL-binding stability, which can be considered to improve ADM targeting to hepatocytes.