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前药-突破递药和靶向障碍的有效途径。

Prodrugs - an efficient way to breach delivery and targeting barriers.

机构信息

School of Pharmacy, University of Eastern Finland, FI-70211 Kuopio, Finland.

出版信息

Curr Top Med Chem. 2011;11(18):2265-87. doi: 10.2174/156802611797183230.

Abstract

The study of prodrugs that are chemically modified bioreversible derivatives of active drug compounds to alter their undesired properties has been expanded widely during the last decades. Despite the commercial success the prodrugs have afforded, the concept is still quite unknown among many scientist. Furthermore, many scientists regard prodrugs as a pure interest of academic research groups and not as a feasible solution to improve the delivery or targeting properties of new chemical entities, drug candidates failed in clinical trials, or drugs withdrawn from the market. Although there are still unmet needs that require addressing, prodrugs should be seen as fine-tuning tools for the successful drug research and development. This review represents the potential of prodrugs to improve the drug delivery by enhanced aqueous solubility or permeability as well as describes several targeted prodrug strategies.

摘要

在过去的几十年中,人们广泛研究了前药,即对活性药物化合物进行化学修饰的生物可逆衍生物,以改变其不良性质。尽管前药取得了商业上的成功,但许多科学家仍然对这个概念知之甚少。此外,许多科学家认为前药只是学术研究小组的兴趣所在,而不是改善新化学实体、临床试验失败的候选药物或从市场上撤出的药物的递送或靶向特性的可行解决方案。尽管仍有未满足的需求需要解决,但前药应该被视为成功进行药物研发的微调工具。这篇综述代表了前药通过提高水溶解度或通透性来改善药物递送的潜力,并描述了几种靶向前药策略。

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