Preparation and Optimization of PEGylated Nano Graphene Oxide-Based Delivery System for Drugs with Different Molecular Structures Using Design of Experiment (DoE)

Molecules. 2021 Mar 7;26(5):1457. doi: 10.3390/molecules26051457.

Abstract

Graphene oxide (GO), due to its 2D planar structure and favorable physical and chemical properties, has been used in different fields including drug delivery. This study aimed to investigate the impact of different process parameters on the average size of drug-loaded PEGylated nano graphene oxide (NGO-PEG) particles using design of experiment (DoE) and the loading of drugs with different molecular structures on an NGO-PEG-based delivery system. GO was prepared from graphite, processed using a sonication method, and functionalized using PEG 6000. Acetaminophen (AMP), diclofenac (DIC), and methotrexate (MTX) were loaded onto NGO-PEG particles. Drug-loaded NGO-PEG was then characterized using dynamic light scattering (DLS), Fourier transform infrared (FTIR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), XRD. The DLS data showed that the drug-loaded NGO-PEG suspensions were in the size range of 200 nm-1.3 µm. The sonication time and the stirring rate were found to be the major process parameters which affected the average size of the drug-loaded NGO-PEG. FTIR, DSC, XRD, and SEM demonstrated that the functionalization or coating of the NGO occurred through physical interaction using PEG 6000. Methotrexate (MTX), with the highest number of aromatic rings, showed the highest loading efficiency of 95.6% compared to drugs with fewer aromatic rings (diclofenac (DIC) 70.5% and acetaminophen (AMP) 65.5%). This study suggests that GO-based nano delivery systems can be used to deliver drugs with multiple aromatic rings with a low water solubility and targeted delivery (e.g., cancer).

Keywords: NGO-PEG; acetaminophen; aromatic ring; diclofenac; graphene oxide (GO); loading efficiency; methotrexate; nano graphene oxide (NGO).

MeSH terms

  • Acetaminophen / administration & dosage
  • Acetaminophen / chemistry
  • Calorimetry, Differential Scanning
  • Diclofenac / administration & dosage
  • Diclofenac / chemistry
  • Drug Carriers / chemistry
  • Drug Delivery Systems / methods*
  • Graphite / chemistry*
  • Methotrexate / administration & dosage
  • Methotrexate / chemistry
  • Microscopy, Electron, Scanning
  • Molecular Structure
  • Nanoparticles / administration & dosage
  • Nanoparticles / chemistry*
  • Particle Size
  • Polyethylene Glycols / chemistry
  • Solubility
  • Spectroscopy, Fourier Transform Infrared
  • X-Ray Diffraction

Substances

  • Drug Carriers
  • graphene oxide
  • Diclofenac
  • Polyethylene Glycol 6000
  • Acetaminophen
  • Polyethylene Glycols
  • Graphite
  • Methotrexate