Endogenous MicroRNA-Triggered and Real-Time Monitored Drug Release via Cascaded Energy Transfer Payloads

Anal Chem. 2017 Oct 3;89(19):10239-10247. doi: 10.1021/acs.analchem.7b01582. Epub 2017 Sep 21.

Abstract

It is a great challenge to design a drug delivery system with a controlled manner, especially one triggered by an exclusive endogenous disease marker and with an easily tracked release process. Herein, we developed a drug delivery platform of carbon dots which were connected to a stem-loop molecular beacon loaded with doxorubicin and polyethylene glycol modified folic acid. Such a platform enables one to release drugs on demand under the stimuli of endogenous microRNA-21, and turn on the fluorescence of carbon dots and doxorubicin, which allows one to monitor the drug release process. The intracellular experiment indicated that folic acid could mediate endocytosis of the nanocarrier, and the overexpressed endogenous microRNA-21 served as a unique key to unlock the drug nanocarrier by competitive hybridization with the molecular beacon, which finally resulted in fluorescence recovery and realized a chemotherapeutic effect within human breast cancer cells. The nanocarrier may have potential application in personalized treatment of different cancer subtypes in which the corresponding miRNAs are overexpressed.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Survival / drug effects
  • Doxorubicin / chemistry
  • Doxorubicin / metabolism*
  • Drug Carriers / chemistry*
  • Drug Carriers / toxicity
  • Drug Liberation
  • Endocytosis
  • Flow Cytometry
  • Fluorescence Resonance Energy Transfer
  • Folic Acid / chemistry
  • Humans
  • MCF-7 Cells
  • MicroRNAs / chemistry*
  • Microscopy, Confocal*
  • Polyethylene Glycols / chemistry
  • Quantum Dots / chemistry
  • Temperature

Substances

  • Drug Carriers
  • MIRN21 microRNA, human
  • MicroRNAs
  • Polyethylene Glycols
  • Doxorubicin
  • Folic Acid