Doxorubicin-conjugated D-glucosamine- and folate- bi-functionalised InP/ZnS quantum dots for cancer cells imaging and therapy

J Drug Target. 2018 Mar;26(3):267-277. doi: 10.1080/1061186X.2017.1365876. Epub 2017 Aug 30.

Abstract

Nanoscaled quantum dots (QDs), with unique optical properties have been used for the development of theranostics. Here, InP/ZnS QDs were synthesised and functionalised with folate (QD-FA), D-glucosamine (QD-GA) or both (QD-FA-GA). The bi-functionalised QDs were further conjugated with doxorubicin (QD-FA-GA-DOX). Optimum Indium to fatty acid (In:MA) ratio was 1:3.5. Transmission electron microscopy (TEM) micrographs revealed spherical morphology for the QDs (11 nm). Energy-dispersive spectroscopy (EDS) spectrum confirmed the chemical composition of the QDs. MTT analysis in the OVCAR-3 cells treated with bare QDs, QD-FA, QD-GA, QD-FA-GA and QD-FA-GA-DOX (0.2 mg/mL of QDs) after 24 h indicated low toxicity for the bare QDs and functionalised QDs (about 80-90% cell viability). QD-FA-GA-DOX nanoparticles elicited toxicity in the cells. Cellular uptake of the engineered QDs were investigated in both folate receptor (FR)-positive OVCAR-3 cells and FR-negative A549 cells using fluorescence microscopy and FACS flow cytometry. The FA-functionalised QDs showed significantly higher uptake in the FR-positive OVCAR-3 cells, nonetheless the GA-functionalised QDs resulted in an indiscriminate uptake in both cell lines. In conclusion, our findings indicated that DOX-conjugated FA-armed QDs can be used as theranostics for simultaneous imaging and therapy of cancer.

Keywords: InP/ZnS quantum dots; folic acid; solid tumours; targeted drug delivery; theranostics.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • A549 Cells
  • Cell Line, Tumor
  • Doxorubicin / administration & dosage
  • Doxorubicin / chemistry*
  • Female
  • Flow Cytometry
  • Folic Acid / administration & dosage
  • Folic Acid / chemistry*
  • Glucosamine / administration & dosage
  • Glucosamine / chemistry*
  • Humans
  • Indium / chemistry
  • Indium / pharmacology
  • Lung Neoplasms / diagnostic imaging*
  • Lung Neoplasms / drug therapy*
  • Ovarian Neoplasms / diagnostic imaging*
  • Ovarian Neoplasms / drug therapy*
  • Phosphines / chemistry
  • Phosphines / pharmacology
  • Quantum Dots / administration & dosage
  • Quantum Dots / chemistry*
  • Sulfides / chemistry
  • Sulfides / pharmacology
  • Zinc Compounds / chemistry
  • Zinc Compounds / pharmacology

Substances

  • Phosphines
  • Sulfides
  • Zinc Compounds
  • Indium
  • Doxorubicin
  • Folic Acid
  • zinc sulfide
  • Glucosamine
  • indium phosphide