Center for Nanotechnology in Drug Delivery, Shiraz University of Medical Sciences, Shiraz, Iran.
Department of Basic Science, Faculty of Veterinary Medicine, University of Tabriz, Tabriz, Iran.
Pharmacol Res. 2020 Jan;151:104551. doi: 10.1016/j.phrs.2019.104551. Epub 2019 Nov 17.
Topoisomerase enzymes have shown unique roles in replication and transcription. These enzymes which were initially found in Escherichia coli have attracted considerable attention as target molecules for cancer therapy. Nowadays, there are several topoisomerase inhibitors in the market to treat or at least control the progression of cancer. However, significant toxicity, low solubility and poor pharmacokinetic properties have limited their wide application and these characteristics need to be improved. Nano-delivery systems have provided an opportunity to modify the intrinsic properties of molecules and also to transfer the toxic agent to the target tissues. These delivery systems leads to the re-introduction of existing molecules present in the market as novel therapeutic agents with different physicochemical and pharmacokinetic properties. This review focusses on a variety of nano-delivery vehicles used for the improvement of pharmacological properties of topoisomerase inhibitors and thus enabling their potential application as novel drugs in the market.
拓扑异构酶在复制和转录中表现出独特的作用。最初在大肠杆菌中发现的这些酶作为癌症治疗的靶分子引起了相当大的关注。如今，市场上有几种拓扑异构酶抑制剂可用于治疗或至少控制癌症的进展。然而，显著的毒性、低溶解度和差的药代动力学特性限制了它们的广泛应用，这些特性需要加以改进。纳米递药系统为修饰分子的固有特性以及将毒性剂递送到靶组织提供了机会。这些递药系统使得现有市场上存在的分子以具有不同理化和药代动力学特性的新型治疗剂重新引入。本综述重点介绍了用于改善拓扑异构酶抑制剂药理特性的各种纳米递药载体，从而使它们有可能作为新型药物在市场上得到应用。
