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Abstract：
Lenvatinib (LVN) is a potentially effective multiple-targeted receptor tyrosine kinase inhibitor approved for treating hepatocellular carcinoma, metastatic renal cell carcinoma and thyroid cancer. Nonetheless, poor pharmacokinetic properties including poor water solubility and rapid metabolic, complex tumor microenvironment, and drug resistance have impeded its satisfactory therapeutic efficacy. This article comprehensively reviews the uses of nanotechnology in LVN to improve antitumor effects. With the characteristic of high modifiability and loading capacity of the nano-drug delivery system, an active targeting approach, controllable drug release, and biomimetic strategies have been devised to deliver LVN to target tumors in sequence, compensating for the lack of passive targeting. The existing applications and advances of LVN in improving therapeutic efficacy include improving longer-term efficiency, achieving higher efficiency, combination therapy, tracking and diagnosing application and reducing toxicity. Therefore, using multiple strategies combined with photothermal, photodynamic, and immunoregulatory therapies potentially overcomes multi-drug resistance, regulates unfavorable tumor microenvironment, and yields higher synergistic antitumor effects. In brief, the nano-LVN delivery system has brought light to the war against cancer while at the same time improving the antitumor effect. More intelligent and multifunctional nanoparticles should be investigated and further converted into clinical applications in the future.
摘要：
Lenvatinib（LVN）是一种潜在有效的多靶向受体酪氨酸激酶抑制剂，被批准用于治疗肝细胞癌，转移性肾细胞癌和甲状腺癌。尽管如此，药代动力学性质差，包括水溶性差和快速代谢，复杂的肿瘤微环境，和耐药性阻碍了其令人满意的治疗效果。本文全面综述了纳米技术在LVN中提高抗肿瘤作用的应用。纳米给药系统具有高的可修饰性和装载能力,积极的瞄准方法，可控药物释放，并且已经设计了仿生策略来将LVN顺序地递送到靶向肿瘤，弥补被动瞄准的不足。LVN在提高治疗效果方面的现有应用和进展包括提高长期效率，实现更高的效率，联合治疗,跟踪和诊断应用，降低毒性。因此,使用多种策略结合光热，光动力，免疫调节疗法有可能克服多药耐药性，调节不利的肿瘤微环境，并产生更高的协同抗肿瘤作用。简而言之,纳米LVN递送系统在提高抗肿瘤效果的同时，为抗癌战争带来了光明。未来应研究更多智能和多功能的纳米颗粒，并进一步转化为临床应用。
