Moxifloxacin loaded nanoparticles of disulfide bridged thiolated chitosan-eudragit RS100 for controlled drug delivery

Int J Biol Macromol. 2021 Jul 1:182:2087-2096. doi: 10.1016/j.ijbiomac.2021.05.199. Epub 2021 Jun 2.

Abstract

The aim of our study was to prepare nanoparticles of disulfide bridged thiolated chitosan and eudragit RS100 using the air oxidation method for controlled drug delivery. The developed nanoparticles were characterized by FTIR, DSC, TGA, zeta sizer, zeta potential, SEM and 1H NMR. The loading, entrapment efficiency and in-vitro release of moxifloxacin from nanoparticles was determined. Toxicity was studied using Caco-2 cell line and pharmacokinetics of moxifloxacin from the developed nanoparticles was studied in albino rats. The FTIR analysis showed no chemical interaction of the drug with the thiolated polymers. The DSC and TGA showed the thermal stability of nanoparticles. The average particle size of nanoparticles was 87 nm, zeta potential of NTC3 was ± 19 and SEM showed the spherical shape of nanoparticles. The 1H NMR spectra confirmed the structure of thiolated chitosan and eudragit RS100. The loading, encapsulation efficiency and release of moxifloxacin from NTC3 were 100.3%, 89.67% and 88.49% respectively. The nanoparticles in culture medium did not affect the viability of Caco-2 cells. The NTC3 formulation showed a greater bioavailability of moxifloxacin compared to the reference formulation. The study reports a convenient and effective way to prepare a chitosan and eudragit RS100 based drug delivery system with a controlled release pattern.

Keywords: Chitosan; Disulfide bridged; Eudragit RS100; Nanoparticles; Thiolation.

MeSH terms

  • Acrylic Resins / chemistry*
  • Animals
  • Caco-2 Cells
  • Calorimetry, Differential Scanning
  • Cell Survival / drug effects
  • Chitosan / chemistry*
  • Delayed-Action Preparations / pharmacology
  • Disulfides / chemistry*
  • Drug Delivery Systems*
  • Drug Liberation
  • Humans
  • Hydrodynamics
  • Kinetics
  • Moxifloxacin / pharmacokinetics
  • Moxifloxacin / pharmacology*
  • Nanoparticles / chemistry*
  • Particle Size
  • Proton Magnetic Resonance Spectroscopy
  • Rats
  • Spectroscopy, Fourier Transform Infrared
  • Static Electricity
  • Sulfhydryl Compounds / chemistry*
  • Thermogravimetry

Substances

  • Acrylic Resins
  • Delayed-Action Preparations
  • Disulfides
  • Sulfhydryl Compounds
  • Eudragit RS
  • Chitosan
  • Moxifloxacin