Journal
ONCOTARGETS AND THERAPY
Volume 11, Issue -, Pages 3257-3265Publisher
DOVE MEDICAL PRESS LTD
DOI: 10.2147/OTT.S165000
Keywords
apatinib microcrystals; radiofrequency ablation; sustained releasing behavior; long-acting efficiency; epithelial-mesenchymal transition; interventional therapy
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Funding
- National Natural Science Foundation of China [81471761, 81501568]
- Tianjin Program to Support Science and Technology Research [15ZCZDSY00890]
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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.
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