Graphene Oxide-Based Nanocomposite for Sustained Release of Cephalexin

J Pharm Sci. 2020 Feb;109(2):1130-1135. doi: 10.1016/j.xphs.2019.09.022. Epub 2019 Sep 27.

Abstract

A sustained-release carrier system for the drug cephalexin (CEF) using functionalized graphene oxide is reported. PEGylation of GO (GO-PEG) and successful loading of CEF into PEGylated graphene oxide (GO-PEG-CEF) nanoconjugate are confirmed by Fourier transform infrared spectroscopy, Raman spectroscopy, and thermogravimetric analysis. Encapsulation efficiency of 69% and a loading capacity of 19% are obtained with the optimized formulation of GO-PEG-CEF. In vitro CEF release profiles show an initial burst release followed by a more sustained release over a 96 h period with cumulative release of 80%. The half maximal inhibitory concentration (IC50) values have both dose- and time-dependent antibacterial activity for GO-PEG-CEF against both gram-positive and gram-negative bacteria while pure CEF showed only dose-dependent antibacterial activity. The minimum inhibitory concentration values of GO-PEG-CEF are 7.8 and 3.9 μg/mL against S. aureus and B. cereus, respectively, while it is 10 μg/mL with pure CEF against both gram-positive bacteria. This confirms the enhanced antibacterial activity of GO-PEG-CEF over pure CEF against gram-positive bacteria. These findings therefore show GO-PEG-CEF is promising as a sustained-release nanoantibiotic system for effective treatment against S. aureus and B. cereus infections.

Keywords: controlled release; drug delivery system(s); drug resistance; graphene; multidrug resistance; nanocomposite(s); nanodrug(s); nanomedicine; nanoparticle(s); nanotechnology.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / pharmacology
  • Cephalexin
  • Delayed-Action Preparations
  • Gram-Negative Bacteria
  • Gram-Positive Bacteria
  • Graphite*
  • Nanocomposites*
  • Staphylococcus aureus

Substances

  • Anti-Bacterial Agents
  • Delayed-Action Preparations
  • graphene oxide
  • Graphite
  • Cephalexin