Antitubercular nanocarrier monotherapy: Study of In Vivo efficacy and pharmacokinetics for rifampicin

J Control Release. 2020 May 10:321:312-323. doi: 10.1016/j.jconrel.2020.02.026. Epub 2020 Feb 14.

Abstract

Tuberculosis represents a major global health problem for which improved approaches are needed to shorten the course of treatment and to combat the emergence of resistant strains. The development of effective and safe nanobead-based interventions can be particularly relevant for increasing the concentrations of antitubercular agents within the infected site and reducing the concentrations in the general circulation, thereby avoiding off-target toxic effects. In this work, rifampicin, a first-line antitubercular agent, was encapsulated into biocompatible and biodegradable polyester-based nanoparticles. In a well-established BALB/c mouse model of pulmonary tuberculosis, the nanoparticles provided improved pharmacokinetics and pharmacodynamics. The nanoparticles were well tolerated and much more efficient than an equivalent amount of free rifampicin.

Keywords: BALB/c mice; Drug delivery system; Histopathology; Nanoparticles; Pharmacokinetics; Rifampicin; Tuberculosis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antibiotics, Antitubercular* / pharmacokinetics
  • Antitubercular Agents
  • Drug Carriers
  • Mice
  • Mice, Inbred BALB C
  • Mycobacterium tuberculosis*
  • Nanostructures
  • Rifampin* / pharmacokinetics
  • Tuberculosis* / drug therapy

Substances

  • Antibiotics, Antitubercular
  • Antitubercular Agents
  • Drug Carriers
  • Rifampin