Nanoparticle-Based Rifampicin Delivery System Development

Molecules. 2021 Apr 3;26(7):2067. doi: 10.3390/molecules26072067.


The alkaline milieu of chronic wounds severely impairs the therapeutic effect of antibiotics, such as rifampicin; as such, the development of new drugs, or the smart delivery of existing drugs, is required. Herein, two innovative polyelectrolyte nanoparticles (PENs), composed of an amphiphilic chitosan core and a polycationic shell, were synthesized at alkaline pH, and in vitro performances were assessed by 1H NMR, elemental analysis, FT-IR, XRD, DSC, DLS, SEM, TEM, UV/Vis spectrophotometry, and HPLC. According to the results, the nanostructures exhibited different morphologies but similar physicochemical properties and release profiles. It was also hypothesized that the simultaneous use of the nanosystem and an antioxidant could be therapeutically beneficial. Therefore, the simultaneous effects of ascorbic acid and PENs were evaluated on the release profile and degradation of rifampicin, in which the results confirmed their synergistic protective effect at pH 8.5, as opposed to pH 7.4. Overall, this study highlighted the benefits of nanoparticulate development in the presence of antioxidants, at alkaline pH, as an efficient approach for decreasing rifampicin degradation.

Keywords: alkaline pH; ascorbic acid; polyelectrolyte nanoparticles; rifampicin.

MeSH terms

  • Calorimetry, Differential Scanning
  • Chromatography, High Pressure Liquid
  • Dextran Sulfate / chemistry
  • Drug Delivery Systems*
  • Drug Liberation
  • Hydrogen-Ion Concentration
  • Nanoparticles / chemistry*
  • Nanoparticles / ultrastructure
  • Particle Size
  • Polyelectrolytes / chemistry
  • Proton Magnetic Resonance Spectroscopy
  • Rifampin / pharmacology*
  • Spectrophotometry, Ultraviolet
  • Spectroscopy, Fourier Transform Infrared
  • Static Electricity
  • X-Ray Diffraction


  • Polyelectrolytes
  • Dextran Sulfate
  • Rifampin