4.8 Article

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

Journal

JOURNAL OF CONTROLLED RELEASE
Volume 321, Issue -, Pages 312-323

Publisher

ELSEVIER
DOI: 10.1016/j.jconrel.2020.02.026

Keywords

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

Funding

  1. Charles University [SVV260440]
  2. Czech Science Foundation [17-07164S, 17-09998S]
  3. Ministry of Education, Youth and Sports of the Czech Republic, National sustainability program I [POLYMAT LO1507]
  4. Research Council of Norway [245942/F50]
  5. Czech Academy of Sciences [TWN-18-10, VAJVA-19-55]

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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.

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