A highly integrated precision nanomedicine strategy to target esophageal squamous cell cancer molecularly and physically

Nanomedicine. 2018 Oct;14(7):2103-2114. doi: 10.1016/j.nano.2018.06.008. Epub 2018 Jul 2.

Abstract

The prognosis of esophageal squamous cell carcinoma is poor. We hereby presented a highly integrated and clinically relevant precision nanomedicine strategy to target ESCC molecularly and physically for significant improvement of the treatment efficacy. We firstly identified PI3K overexpression in patient samples and its relation to poor patient survival. With our highly versatile tumor-targeted drug delivery platform (DCM), we were able to load a potent but toxic docetaxel (DTX) and a PI3K inhibitor (AZD8186) with favorable physical properties. The combination of the DTX-DCM and AZD8186-DCM showed a highly efficacious and synergistic anti-tumor effect and decreased hematotoxicity. A pro-apoptotic protein, Bax was significantly upregulated in ESCC cells treated with combination therapy compared to that with monotherapy. This study utilized a highly integrated precision nano-medicine strategy that combines the identification of cancer molecular target from human patients, precision drug delivery and effective combination therapy for the development of better ESCC treatment.

Keywords: Docetaxel; Esophageal squamous cell carcinoma; Nanoparticle; PI3K inhibitor; Precision nanomedicine.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aniline Compounds / pharmacology*
  • Animals
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology
  • Apoptosis
  • Biomarkers, Tumor / metabolism
  • Carcinoma, Squamous Cell / drug therapy*
  • Carcinoma, Squamous Cell / metabolism
  • Carcinoma, Squamous Cell / pathology
  • Cell Proliferation
  • Chromones / pharmacology*
  • Class I Phosphatidylinositol 3-Kinases / antagonists & inhibitors*
  • Class I Phosphatidylinositol 3-Kinases / metabolism
  • Docetaxel / administration & dosage
  • Docetaxel / chemistry
  • Docetaxel / pharmacology*
  • Drug Delivery Systems*
  • Drug Therapy, Combination
  • Esophageal Neoplasms / drug therapy*
  • Esophageal Neoplasms / metabolism
  • Esophageal Neoplasms / pathology
  • Female
  • Humans
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Mice, Nude
  • Middle Aged
  • Nanomedicine*
  • Neoplasm Invasiveness
  • Prognosis
  • Tumor Cells, Cultured
  • Xenograft Model Antitumor Assays

Substances

  • AZD8186
  • Aniline Compounds
  • Antineoplastic Agents
  • Biomarkers, Tumor
  • Chromones
  • Docetaxel
  • Class I Phosphatidylinositol 3-Kinases
  • PIK3CA protein, human