a Institute for Maternal and Child Health , IRCCS Burlo Garofolo , Trieste , Italy.
b Department of Morphology, Surgery, Experimental Medicine and LTTA Centre , University of Ferrara , Ferrara , Italy.
Expert Opin Drug Deliv. 2019 May;16(5):481-496. doi: 10.1080/17425247.2019.1604679. Epub 2019 May 2.
Progressive breakthroughs in nanomedicine have been instrumental for the clinical translation of actively targeted drug-delivery approaches. Besides storing large payloads of drugs within the nanoparticle core, the conjugation of targeting moieties confers specific targeting ability to the nanoplatforms. In this respect, clinical results suggest that actively targeted nanocarriers can exhibit an overall improved antitumor efficacy, minimizing off-target toxicity.
This review article summarizes the advances in active targeting of nanocarriers to cancer cells. Specifically, we discuss the various types of nanocarriers, describe the receptors that are frequently overexpressed in solid tumors, and discuss how this approach can be used to improve clinical outcomes. We particularly focus on ongoing clinical trials of actively targeted nanoparticles that are yet to be clinically approved.
Further investment in active targeting will likely pose clinical benefits. We envisage a future requiring the use of longitudinal measures in the clinical setting to profile the patients that are likely to benefit from actively targeted nanocarriers. At the preclinical stage, a complete picture of intratumoral barriers combined with a quantitative approach of the intratumoral fate of nanomaterials will be instrumental in defining more effective strategies to improve their clinical translation.
纳米医学的突破性进展对于主动靶向药物传递方法的临床转化至关重要。除了在纳米颗粒核心内储存大量药物负载外,靶向部分的缀合还赋予纳米平台特定的靶向能力。在这方面,临床结果表明,主动靶向纳米载体可以表现出整体改善的抗肿瘤疗效,最大程度地减少非靶毒性。
本文综述了主动靶向纳米载体对癌细胞的研究进展。具体来说,我们讨论了各种类型的纳米载体,描述了在实体瘤中经常过度表达的受体,并讨论了如何利用这种方法来改善临床结果。我们特别关注正在进行的尚未获得临床批准的主动靶向纳米粒子的临床试验。
对主动靶向的进一步投资可能会带来临床益处。我们设想未来需要在临床环境中使用纵向措施来对可能受益于主动靶向纳米载体的患者进行分析。在临床前阶段,结合对纳米材料在肿瘤内命运的定量方法,全面了解肿瘤内的屏障将有助于确定更有效的策略,以改善其临床转化。