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适配体作为药物递送载体。

Aptamers as drug delivery vehicles.

作者信息

Kruspe Sven, Mittelberger Florian, Szameit Kristina, Hahn Ulrich

机构信息

Institut für Biochemie und Molekularbiologie, Universität Hamburg, Martin-Luther-King Platz 6, 20146 Hamburg (Germany).

出版信息

ChemMedChem. 2014 Sep;9(9):1998-2011. doi: 10.1002/cmdc.201402163. Epub 2014 Aug 11.

Abstract

The benefits of directed and selective therapy for systemic treatment are reasons for increased interest in exploiting aptamers for cell-specific drug delivery. Nucleic acid based pharmaceuticals represent an interesting and novel tool to counter human diseases. Combining inhibitory potential and cargo transfer upon internalization, nanocarriers as well as various therapeutics including siRNAs, chemotherapeutics, photosensitizers, or proteins can be imported via these synthetic nucleic acids. However, widespread clinical application is still hampered by obstacles that must be overcome. In this review, we give an overview of applications and recent advances in aptamer-mediated drug delivery. We also introduce prominent selection methods as well as useful approaches in choice of drug and conjugation method. We discuss the challenges that need to be considered and present strategies that have been applied to achieve intracellular delivery of effectors transported by readily internalized aptamers.

摘要

定向和选择性疗法用于全身治疗的益处,是人们对利用适配体进行细胞特异性药物递送兴趣增加的原因。基于核酸的药物是对抗人类疾病的一种有趣且新颖的工具。纳米载体以及包括小干扰RNA、化疗药物、光敏剂或蛋白质在内的各种治疗剂,可通过这些合成核酸导入,它们在内化后兼具抑制潜力和货物转运能力。然而,广泛的临床应用仍受到一些必须克服的障碍的阻碍。在本综述中,我们概述了适配体介导的药物递送的应用和最新进展。我们还介绍了突出的筛选方法以及药物选择和偶联方法中的有用方法。我们讨论了需要考虑的挑战,并介绍了为实现由易于内化的适配体转运的效应物的细胞内递送而应用的策略。

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