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Strategies and challenges to improve the performance of tumor-associated active targeting.
Journal of Materials Chemistry B ( IF 6.1 ) Pub Date : 2020-05-14 , DOI: 10.1039/d0tb00289e Yahui Zhang 1 , Jing Cao 1 , Zhi Yuan 2
Journal of Materials Chemistry B ( IF 6.1 ) Pub Date : 2020-05-14 , DOI: 10.1039/d0tb00289e Yahui Zhang 1 , Jing Cao 1 , Zhi Yuan 2
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Over the past decade, nanoparticle-based drug delivery systems have been extensively explored. However, the average tumour enrichment ratio of passive targeting systems corresponds to only 0.7% due to the nonspecific uptake by normal organs and poor selective retention in tumours. The therapeutic specificity and efficacy of nano-medicine can be enhanced by equipping it with active targeting ligands, although it is not possible to ignore the recognition and clearance of the reticuloendothelial system (RES) caused by targeting ligands. Given the complexity of the systemic circulation environment, it is necessary to carefully consider the hydrophobicity, immunogenicity, and electrical property of targeting ligands. Thus, for an active targeting system, the targeting ligands should be shielded in blood circulation and de-shielded in the tumour region for enhanced tumour accumulation. In this study, strategies for improving the performance of active targeting ligands are introduced. The strategies include irreversible shielding, reversible shielding, and methods of modulating the multivalent interactions between ligands and receptors. Furthermore, challenges and future developments in designing active ligand targeting systems are also discussed.
中文翻译：
改善肿瘤相关主动靶向治疗的策略和挑战。
在过去的十年中，已经广泛探索了基于纳米颗粒的药物递送系统。然而，由于正常器官的非特异性吸收和不良的肿瘤选择性保留，被动靶向系统的平均肿瘤富集率仅相当于0.7％。通过配备活性靶向配体可以增强纳米药物的治疗特异性和功效，尽管不可能忽略由靶向配体引起的网状内皮系统（RES）的识别和清除。考虑到全身循环环境的复杂性，有必要仔细考虑靶向配体的疏水性，免疫原性和电性能。因此，对于主动定位系统，靶向配体应在血液循环中被屏蔽，并在肿瘤区域中被屏蔽，以增强肿瘤的积累。在这项研究中，介绍了改善活性靶向配体性能的策略。这些策略包括不可逆屏蔽，可逆屏蔽以及调节配体和受体之间多价相互作用的方法。此外，还讨论了设计活性配体靶向系统的挑战和未来发展。
更新日期：2020-03-06
中文翻译：
改善肿瘤相关主动靶向治疗的策略和挑战。
在过去的十年中，已经广泛探索了基于纳米颗粒的药物递送系统。然而，由于正常器官的非特异性吸收和不良的肿瘤选择性保留，被动靶向系统的平均肿瘤富集率仅相当于0.7％。通过配备活性靶向配体可以增强纳米药物的治疗特异性和功效，尽管不可能忽略由靶向配体引起的网状内皮系统（RES）的识别和清除。考虑到全身循环环境的复杂性，有必要仔细考虑靶向配体的疏水性，免疫原性和电性能。因此，对于主动定位系统，靶向配体应在血液循环中被屏蔽，并在肿瘤区域中被屏蔽，以增强肿瘤的积累。在这项研究中，介绍了改善活性靶向配体性能的策略。这些策略包括不可逆屏蔽，可逆屏蔽以及调节配体和受体之间多价相互作用的方法。此外，还讨论了设计活性配体靶向系统的挑战和未来发展。
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