Mucoadhesive chitosan-coated solid lipid nanoparticles for better management of tuberculosis

Int J Pharm. 2018 Jan 30;536(1):478-485. doi: 10.1016/j.ijpharm.2017.11.071. Epub 2017 Dec 2.

Abstract

Taking into consideration the potential mucoadhesion properties of systems in lung delivery, this paper describes the preparation and characterization of chitosan-coated solid lipid nanoparticles (C-SLNs) loaded with rifampicin (RIF) as anti-tuberculosis (anti-TB) drug. The process of development and characterization of the NPs in terms of size, surface charge, encapsulation efficiency (EE), morphology, in vitro drug release, differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), in vitro assessment of mucoadhesive property, cell viability and permeability studies are documented. Results showed that the SLNs had a smooth spherical shape with a size of ca. 245-344 nm and with a zeta potential around -30 mV for SLNs and +40 mV for C-SLNs. The surface charge variation from negative to positive charge and FTIR analysis demonstrated the successful process of coating the nanoparticles (NPs) surface with chitosan. The DSC thermograms were in agreement with the nanostructure of the SLNs. The EE of drug was found to be higher than 90% and the loading capacity (LC) around 4.5%. C-SLNs show higher in vitro muchoadesive properties and a higher permeability in alveolar epithelial cells A549 than uncoated SLNs, indicating that the developed C-SLNs can be used as a promising carrier for sasfer and efficient management of TB.

Keywords: Adsorption; Chitosan; Macrophages; Mucoadhesion; Tuberculosis.

MeSH terms

  • Antitubercular Agents / administration & dosage*
  • Antitubercular Agents / chemistry*
  • Chitosan / chemistry*
  • Drug Carriers / chemistry
  • Drug Liberation / drug effects
  • Excipients / chemistry
  • Lipids / chemistry*
  • Nanoparticles / chemistry*
  • Nanostructures / chemistry
  • Particle Size
  • Rifampin / administration & dosage
  • Rifampin / chemistry
  • Tuberculosis / drug therapy*

Substances

  • Antitubercular Agents
  • Drug Carriers
  • Excipients
  • Lipids
  • Chitosan
  • Rifampin