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

Journal of controlled release : official journal of the Controlled Release Society, Volume: 321
May 10, 2020
Jiří Trousil J, Oto Pavliš O, Pavla Kubíčková P, Miša Škorič M, Věra Marešová V, Ewa Pavlova E, Kenneth D Knudsen KD, You-Shan Dai YS, Matthew Zimmerman M, Véronique Dartois V, Jia-You Fang JY, Martin Hrubý M

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.