Doxorubicin (DOX)-loaded glycyrrhetinic acid (GA)-modified alginate (ALG) nanoparticles (DOX/GA-ALG NPs) were prepared for targeting therapy of liver cancer. This study focused on the biodistribution of DOX/GA-ALG NPs in Kunming mice as well as their antitumor activity against liver tumors in situ and side effects. The biodistribution data showed that the concentration of DOX in the liver reached 67.8 ± 4.9 μg/g after intravenous administration of DOX/GA-ALG NPs, which was 2.8-fold and 4.7-fold higher compared to non-GA-modified nanoparticles (DOX/CHO-ALG NPs) and DOX·HCl, respectively. The concentration of DOX in the heart of mice treated with DOX/GA-ALG NPs at any sampling time was relatively lower than that of mice treated with DOX·HCl. The liver tumor growth inhibition rate (IR) in situ was about 52.6% and the mortality was 33% in DOX·HCl group. In contrast, the IR was 76.6% and no mice died in the DOX/GA-ALG NPs group. Histological examination showed tumor necrosis in both experimental groups. Most importantly, the heart cells and the liver cells surrounding the tumor were not affected by administration of DOX/GA-ALG NPs, whereas myocardial necrosis and apparent liver cell swelling were observed after DOX·HCl administration.
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