A new apatinib microcrystal formulation enhances the effect of radiofrequency ablation treatment on hepatocellular carcinoma

Hui Xie, Shengtao Tian, Haipeng Yu, Xueling Yang, Jia Liu, Huaming Wang, Fan Feng, Zhi Guo

    Research output: Contribution to journalArticle

    20 Scopus citations


    Introduction: Radiofrequency ablation (RFA) is the foremost treatment option for advanced hepatocellular carcinoma (HCC), however, rapid and aggressive recurrence of HCC often occurs after RFA due to epithelial–mesenchymal transition process. Although combination of RFA with sorafenib, a molecular targeted agent, could attenuate the recurrence of HCC, application of this molecular targeted agent poses a heavy medical burden and oral administration of sorafenib also brings severe side effects. Materials and methods: In this study, we prepared an apatinib microcrystal formulation (Apa-MS) that sustainably releases apatinib, a novel molecular targeted agent, for advanced HCC treatment. We injected apatinib solution or Apa-MS into subcutaneous HCC tumors. Results: It was found that Apa-MS exhibited slow apatinib release in vivo and in turn inhibited the epithelial–mesenchymal transition of HCC cells for extended time. Moreover, in rodent HCC model, Apa-MS enhanced the antitumor effect of RFA treatment. Conclusion: Based on these results, we conclude that Apa-MS, a slow releasing system of apatinib, allows apatinib to remain effective in tumor tissues for a long time and could enhance the antitumor effect of RFA on HCC.

    Original languageEnglish (US)
    Pages (from-to)3257-3265
    Number of pages9
    JournalOncoTargets and Therapy
    StatePublished - May 31 2018



    • Apatinib microcrystals
    • Epithelial-mesenchymal transition
    • Interventional therapy
    • Longacting efficiency
    • Radiofrequency ablation
    • Sustained releasing behavior

    ASJC Scopus subject areas

    • Oncology
    • Pharmacology (medical)

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