Currently, limited tumor drug permeation and poor oxygen perfusion are two major bottlenecks that significantly impair the efficacy of existing antitumor drugs, especially oxygen‐sensitive antitumor drugs. One vital cause of these major bottlenecks is the abnormal tumor vessel barrier. To the best knowledge of the authors, platelets play a vital role in the maintenance of an abnormal tumor blood barrier through platelet–tumor interaction. Thus, platelet inhibition may present a new way to enhance drug delivery. In this study, it is originally discovered that perfluorotributylamine‐based albumin nanoparticles (PFTBA@HSA) possess excellent platelet inhibiting abilities, which then selectively disrupt the tumor vessel barrier, resulting in a remarkably enhanced intratumoral drug accumulation. Interestingly enough, the tumor hypoxia is also obviously relieved by enhanced oxygen carrier red blood cell distribution and PFTBA@HSA infiltration in the tumors. Finally, the efficacy of oxygen‐sensitive antitumor drugs is significantly amplified by PFTBA@HSA owing to enhanced drug permeation and relieved tumor hypoxia. Therefore, for the first time, it is demonstrated that PFTBA@HSA could be used as an effective way to improve the efficacy of existing tumor therapies by disrupting tumor vessel barriers through targeted platelet inhibition.

中文翻译：

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全氟化碳纳米颗粒介导的血小板阻断破坏血管屏障，以提高对氧敏感的抗肿瘤药物的功效

当前，有限的肿瘤药物渗透和不良的氧灌注是严重损害现有抗肿瘤药物，特别是对氧敏感的抗肿瘤药物的功效的两个主要瓶颈。这些主要瓶颈的一个重要原因是异常的肿瘤血管屏障。据作者所知，血小板通过血小板与肿瘤的相互作用在维持异常的肿瘤血液屏障中起着至关重要的作用。因此，血小板抑制可能是增强药物输送的新途径。在这项研究中，最初发现基于全氟三丁胺的白蛋白纳米颗粒（PFTBA @ HSA）具有出色的血小板抑制能力，然后选择性地破坏肿瘤血管屏障，导致肿瘤内药物蓄积显着增强。有趣的是，氧载体红细胞分布的增强和PFTBA @ HSA在肿瘤中的浸润也明显缓解了肿瘤的缺氧。最后，由于提高了药物的渗透性并减轻了肿瘤的缺氧，PFTBA @ HSA大大增强了对氧敏感的抗肿瘤药物的疗效。因此，首次证明了PFTBA @ HSA可以作为通过靶向血小板抑制破坏肿瘤血管屏障来提高现有肿瘤疗法疗效的有效方法。