Section of Medicinal and Cosmetic Chemistry, Department of Pharmacy, University of Genova, Viale Benedetto XV, 3-16132 Genova, Italy.
Int J Mol Sci. 2021 Jun 18;22(12):6538. doi: 10.3390/ijms22126538.
Nanotechnology is an important application in modern cancer therapy. In comparison with conventional drug formulations, nanoparticles ensure better penetration into the tumor mass by exploiting the enhanced permeability and retention effect, longer blood circulation times by a reduced renal excretion and a decrease in side effects and drug accumulation in healthy tissues. The most significant classes of nanoparticles (i.e., liposomes, inorganic and organic nanoparticles) are here discussed with a particular focus on their use as delivery systems for small molecule tyrosine kinase inhibitors (TKIs). A number of these new compounds (e.g., Imatinib, Dasatinib, Ponatinib) have been approved as first-line therapy in different cancer types but their clinical use is limited by poor solubility and oral bioavailability. Consequently, new nanoparticle systems are necessary to ameliorate formulations and reduce toxicity. In this review, some of the most important TKIs are reported, focusing on ongoing clinical studies, and the recent drug delivery systems for these molecules are investigated.
纳米技术是现代癌症治疗中的一个重要应用。与传统药物制剂相比，纳米颗粒通过利用增强的通透性和保留效应更好地渗透到肿瘤组织中，通过减少肾脏排泄而延长血液循环时间，并减少副作用和药物在健康组织中的积累。这里讨论了最显著的纳米颗粒类别（即脂质体、无机和有机纳米颗粒），特别关注它们作为小分子酪氨酸激酶抑制剂 (TKI) 的递送系统的用途。许多这些新化合物（例如伊马替尼、达沙替尼、泊那替尼）已被批准用于不同类型的癌症的一线治疗，但由于其溶解度差和口服生物利用度低，其临床应用受到限制。因此，需要新的纳米颗粒系统来改善制剂并降低毒性。在这篇综述中，报告了一些最重要的 TKI，重点介绍了正在进行的临床研究，并研究了这些分子的最近药物递送系统。
