Nanoformulated paclitaxel and AZD9291 synergistically eradicate non-small-cell lung cancers in vivo

Nanomedicine (Lond). 2018 May;13(10):1107-1120. doi: 10.2217/nnm-2017-0355. Epub 2018 Jun 6.

Abstract

Aim: This study aims to develop new nanoformulations of EGFR T790M targeted inhibitor AZD9291 and paclitaxel (PTX) for combination therapy of lung cancer.

Materials & methods: We prepared and characterized PTX- and AZD9291-loaded disulfide cross-linking micelles (DCMs), and evaluate their combination effect and toxicity in vitro and in lung cancer-bearing mice.

Results: Drug-loaded DCMs were relatively small in size, and possessed glutathione-responsive drug release. The combination of PTX-DCMs and AZD92921-DCMs exhibited strong synergistic effects in both cell line and in vivo without additional toxicity. Molecular studies demonstrated the synergistic modification in both IKB-α/NF-κB/Bcl-2 and EGFR/Akt pathways.

Conclusion: The combination of DCM-loaded AZD9291 and PTX could potentially offer more effective and less toxicity treatment options for lung cancer patients.

Keywords: AZD9291; EGFR inhibitor; NSCLC; paclitaxel.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Acrylamides / administration & dosage*
  • Acrylamides / chemistry
  • Aniline Compounds / administration & dosage*
  • Aniline Compounds / chemistry
  • Animals
  • Apoptosis / drug effects
  • Carcinoma, Non-Small-Cell Lung / chemistry
  • Carcinoma, Non-Small-Cell Lung / drug therapy*
  • Carcinoma, Non-Small-Cell Lung / pathology
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Drug Delivery Systems*
  • Drug Liberation
  • Drug Resistance, Neoplasm / genetics
  • Humans
  • Mice
  • Paclitaxel / administration & dosage*
  • Paclitaxel / chemistry
  • Xenograft Model Antitumor Assays

Substances

  • Acrylamides
  • Aniline Compounds
  • osimertinib
  • Paclitaxel