纳米粒子对肿瘤的主动靶向是纳米医学中发展最迅速的课题之一。通常,这种策略涉及在纳米粒子中添加靶向癌症的生物分子,关于这一主题的研究主要集中在此类制剂在肿瘤中的定位上。这里,分析决定有效纳米粒子靶向和治疗的因素,各种参数,如靶向分子的类型,纳米粒子类型,尺寸,zeta电位,剂量,并给出了循环时间。此外,讨论了重要的方面,例如纳米颗粒的主动靶向如何改变生物分布以及非特异性器官摄取如何影响靶向纳米制剂的肿瘤积累。分析揭示了靶向纳米颗粒的肿瘤积累的增加伴随着它们被脾吸收的减少。在肿瘤和其他器官中靶向诱导的纳米颗粒浓度变化之间没有关联。与裸鼠相比,对于具有完整免疫系统的小鼠,肿瘤中的摄取与脾脏中的消耗之间的相关性很重要。值得注意的是,脾和肿瘤积累的调节取决于靶向分子和纳米颗粒类型。中位生存期随着靶向诱导的纳米颗粒在肿瘤中的积累而增加;此外,纳米颗粒药物的组合靶向显示出更高的治疗效率。综合分析的结果表明了提高主动靶向纳米颗粒药物效率的最佳策略。
Active targeting of nanoparticles toward tumors is one of the most rapidly developing topics in nanomedicine. Typically, this strategy involves the addition of cancer-targeting biomolecules to nanoparticles, and studies on this topic have mainly focused on the localization of such formulations in tumors. Here, the analysis of the factors determining efficient nanoparticle targeting and therapy, various parameters such as types of targeting molecules, nanoparticle type, size, zeta potential, dose, and the circulation time are given. In addition, the important aspects such as how active targeting of nanoparticles alters biodistribution and how non-specific organ uptake influences tumor accumulation of the targeted nanoformulations are discussed. The analysis reveals that an increase in tumor accumulation of targeted nanoparticles is accompanied by a decrease in their uptake by the spleen. There is no association between targeting-induced changes of nanoparticle concentrations in tumors and other organs. The correlation between uptake in tumors and depletion in the spleen is significant for mice with intact immune systems in contrast to nude mice. Noticeably, modulation of splenic and tumor accumulation depends on the targeting molecules and nanoparticle type. The median survival increases with the targeting-induced nanoparticle accumulation in tumors; moreover, combinatorial targeting of nanoparticle drugs demonstrates higher treatment efficiencies. Results of the comprehensive analysis show optimal strategies to enhance the efficiency of actively targeted nanoparticle-based medicines.