Lipid nanoparticles coated with chitosan using a one-step association method to target rifampicin to alveolar macrophages

Carbohydr Polym. 2021 Jan 15:252:116978. doi: 10.1016/j.carbpol.2020.116978. Epub 2020 Sep 24.

Abstract

This work proposes the development and characterization of solid lipid nanoparticles (SLNs) loaded with rifampicin (RIF) aiming to enhance mucoadhesion of the SLNs and consequently internalization by the alveolar macrophages (AMs). The lipid nanoparticles (NPs) were characterized and the results showed that the NPs obtained present a spherical or a starry shape with diameter around 250-500 nm, a monodisperse population, with zeta potential between -31 mV for uncoated SLNs and +33 mV for coated SLNs. The drug EE was approximately 90 % and the loading capacity (LC) 4.5 %. The SLNs coated with chitosan by the association method (aC-SLNs) show an effective mucoadhesive profile, verified by the turdimetry and surface loading method, corroborated with the cellular assays. The presence of chitosan in the aC-SLNs promotes higher mucoadhesive properties to the NPs and permeability in A549, suggesting that the safe aC-SLNs-RIF can be used as a promising drug delivery system for improving tuberculosis treatment.

Keywords: Alveolar epithelial cells; Association method; Chitosan; Infection; Mucoadhesion; Nanomedicine; Rifampicin.

MeSH terms

  • A549 Cells
  • Antibiotics, Antitubercular / administration & dosage*
  • Chitosan / chemistry*
  • Drug Carriers / chemistry*
  • Drug Liberation
  • Humans
  • Lipids / chemistry*
  • Macrophages, Alveolar / drug effects*
  • Nanoparticles / chemistry*
  • Particle Size
  • Rifampin / administration & dosage*
  • Tuberculosis / drug therapy

Substances

  • Antibiotics, Antitubercular
  • Drug Carriers
  • Lipids
  • Chitosan
  • Rifampin