文章：

药物从血管到肿瘤组织的运输

Transport of drugs from blood vessels to tumour tissue

原文发布日期：2017-12-01

DOI: 10.1038/nrc.2017.93

类型: Review Article

开放获取: 否

要点：

1. The transport of anticancer drugs throughout all regions of a solid tumour is a crucial factor in the effectiveness of the drug.
2. Generally, drugs are delivered by convection in the blood and then permeate vessel walls and penetrate the surrounding tissue by diffusion or convection.
3. The distribution of drug in tumour tissue is strongly influenced by the structure and function of the tumour vasculature, which typically has aberrant properties. The abnormal properties of the extracellular matrix in the tumour tissue can also limit drug distribution.
4. Physical properties of the drug, including size, charge, lipid solubility and surface properties (for nanoparticles), have major effects on the transport of the drug to tissue. The penetration distance of the drug into tissue also depends on solute binding and uptake rates in the tissue.
5. A number of methods have been developed for overcoming limitations in drug transport and thereby achieving improved therapeutic results.
6. In the design and usage of drugs, increased attention to transport properties has the potential to result in better treatments for solid tumours.

要点翻译：

1. 抗癌药物在实体瘤所有区域的传输是影响药物疗效的关键因素。
2. 通常，药物通过血液中的对流输送，然后通过扩散或对流渗透血管壁并进入周围组织。
3. 药物在肿瘤组织中的分布受到肿瘤血管结构和功能的显著影响，这些血管通常具有异常特性。肿瘤组织中细胞外基质的异常特性也可能限制药物的分布。
4. 药物的物理特性，包括大小、电荷、脂溶性及表面性质（对纳米颗粒而言），对药物向组织的传输具有重要影响。药物在组织中的渗透距离还取决于溶质在组织中的结合和摄取速率。
5. 目前已开发多种方法用于克服药物传输的局限性，从而实现更好的治疗效果。
6. 在药物的设计和使用过程中，对传输特性的日益关注有望为实体瘤带来更有效的治疗方法。

英文摘要：

The effectiveness of anticancer drugs in treating a solid tumour is dependent on delivery of the drug to virtually all cancer cells in the tumour. The distribution of drug in tumour tissue depends on the plasma pharmacokinetics, the structure and function of the tumour vasculature and the transport properties of the drug as it moves through microvessel walls and in the extravascular tissue. The aim of this Review is to provide a broad, balanced perspective on the current understanding of drug transport to tumour cells and on the progress in developing methods to enhance drug delivery. First, the fundamental processes of solute transport in blood and tissue by convection and diffusion are reviewed, including the dependence of penetration distance from vessels into tissue on solute binding or uptake in tissue. The effects of the abnormal characteristics of tumour vasculature and extravascular tissue on these transport properties are then discussed. Finally, methods for overcoming limitations in drug transport and thereby achieving improved therapeutic results are surveyed.

摘要翻译： 

抗癌药物治疗实体瘤的效果，取决于药物是否能送达肿瘤内几乎所有癌细胞。药物在肿瘤组织中的分布，取决于血浆药代动力学、肿瘤血管的结构与功能，以及药物穿过微血管壁和在血管外组织中移动的转运特性。本综述旨在全面、平衡地阐述目前对药物向肿瘤细胞转运机制的理解，以及在增强药物递送方法上的进展。首先，回顾溶质在血液和组织中通过对流和扩散进行转运的基本过程，包括溶质在组织中的结合或摄取如何影响其从血管进入组织的渗透距离。随后，讨论肿瘤血管和血管外组织的异常特征对这些转运特性的影响。最后，概述克服药物转运限制、从而实现更佳治疗效果的策略。

原文链接：

Transport of drugs from blood vessels to tumour tissue