Topoisomerase inhibitors: Pharmacology and emerging nanoscale delivery systems

Pharmacol Res. 2020 Jan:151:104551. doi: 10.1016/j.phrs.2019.104551. Epub 2019 Nov 17.

Abstract

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.

Keywords: Cancer; Chemotherapy; Drug delivery systems; Nanocarriers; Nanoparticles; Topoisomerase inhibitors.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • DNA Topoisomerases / metabolism
  • Drug Delivery Systems* / methods
  • Humans
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism
  • Topoisomerase Inhibitors / administration & dosage
  • Topoisomerase Inhibitors / pharmacology
  • Topoisomerase Inhibitors / therapeutic use*

Substances

  • Antineoplastic Agents
  • Topoisomerase Inhibitors
  • DNA Topoisomerases