Targeted macrophages delivery of rifampicin-loaded lipid nanoparticles to improve tuberculosis treatment

Nanomedicine (Lond). 2017 Dec;12(24):2721-2736. doi: 10.2217/nnm-2017-0248. Epub 2017 Nov 9.

Abstract

Aim: This work aims to develop a mannosylated nanostructured lipid carrier (NLC) loaded with rifampicin to improve tuberculosis treatment.

Materials & methods: An active targeting strategy was used and the nanoparticles were characterized. Effects on cell viability and the antimycobacterial activity of the nanoformulations were evaluated.

Results: The nanoparticles developed exhibited a size of about 315 nm and polydispersity <0.2. The drug encapsulation efficiency was higher than 90% and its release was sensitive to pH. The mannosylated NLCs showed efficient uptake by bone marrow derived macrophages. Further, rifampicin-loaded mannosylated NLCs were more efficient in inducing a decrease of intracellular growth of mycobacteria.

Conclusion: The NLCs developed can be used as a promising carrier for safer and efficient management of tuberculosis.

Keywords: Mycobacterium tuberculosis; active targeting; drug delivery; infectious diseases; nanomedicine.

MeSH terms

  • Animals
  • Antibiotics, Antitubercular / chemistry
  • Antibiotics, Antitubercular / pharmacology*
  • Biological Transport
  • Cell Survival
  • Drug Carriers / chemistry*
  • Drug Liberation
  • Female
  • Humans
  • Hydrogen-Ion Concentration
  • Lipids / chemistry*
  • Macrophages / cytology
  • Macrophages / drug effects*
  • Macrophages / microbiology
  • Mannose / chemistry
  • Mice, Inbred C57BL
  • Mycobacterium avium / drug effects*
  • Mycobacterium avium / isolation & purification
  • Nanoparticles / chemistry*
  • Particle Size
  • Rifampin / chemistry
  • Rifampin / pharmacology*
  • Surface Properties
  • Tuberculosis, Pulmonary / drug therapy*

Substances

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