Be Active or Not: the Relative Contribution of Active and Passive Tumor Targeting of Nanomaterials.
Be Active or Not: the Relative Contribution of Active and Passive Tumor Targeting of Nanomaterials.
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主动与否：纳米材料主动和被动肿瘤靶向的相对贡献。
DOI：
10.7150/ntno.19380
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发表时间：
2017
期刊：
影响因子：
--
通讯作者：
Huang M
中科院分区：
文献类型：
--
作者：
Li R;Zheng K;Yuan C;Chen Z;Huang M
恶性肿瘤（癌症）仍然是世界上最致命的疾病之一，尽管其总体死亡率下降。纳米材料（NM）已被广泛研究作为肿瘤的诊断和/或治疗剂。与小分子相比，NM的一个特征是NM可以通过增强的渗透性和保留（EPR）效应被动地集中在肿瘤中。同时，NM可以被工程化以以主动方式靶向肿瘤特异性标志物，例如，受体介导的靶向。EPR效应和受体介导的靶向对肿瘤组织中NM积累的相对贡献尚未明确定义。在这里，我们通过回顾以前的研究来解决这个基本问题。首先，我们总结了目前的知识，这两个肿瘤靶向策略的纳米粒子，以及纳米粒子如何到达肿瘤的血液循环。然后，我们证明了主动和被动效应对肿瘤中NM总积累的贡献随时间而变化。随着时间的推移，在尿激酶型纤溶酶原激活物受体（uPAR）介导的靶向和人血清白蛋白（HSA）介导的EPR效应的情况下，受体介导的靶向比EPR效应贡献更多，比率为3。因此，本文综述了NMs在肿瘤部位积累的主动和被动靶向动力学，对未来NMs在癌症诊断和治疗中的设计具有价值。
Malignant tumor (cancer) remains as one of the deadliest diseases throughout the world, despite its overall mortality drops. Nanomaterials (NMs) have been widely studied as diagnostic and/or therapeutic agents for tumors. A feature of NMs, compared to small molecules, is that NMs can be concentrated passively in tumors through enhanced permeability and retention (EPR) effect. In the meantime, NMs can be engineered to target toward tumor specific markers in an active manner, e.g., receptor-mediated targeting. The relative contribution of the EPR effect and the receptor-mediated targeting to NM accumulation in tumor tissues has not been clearly defined yet. Here, we tackle this fundamental issue by reviewing previous studies. First, we summarize the current knowledge on these two tumor targeting strategies of NMs, and on how NMs arrive to tumors from blood circulation. We then demonstrate that contribution of the active and passive effects to total accumulation of NMs in tumors varies with time. Over time, the receptor-mediated targeting contributes more than the EPR effect with a ratio of 3 in the case of urokinase-type plasminogen activator receptor (uPAR)-mediated targeting and human serum albumin (HSA)-mediated EPR effect. Therefore, this review highlights the dynamics of active and passive targeting of NMs on their accumulation at tumor sites, and is valuable for future design of NMs in cancer diagnosis and treatment.