Institute of Macromolecular Chemistry, Czech Academy of Sciences, Heyrovského náměstí 2, 162 00 Prague 6, Czechia; Department of Analytical Chemistry, Faculty of Science, Charles University, Hlavova 8, 128 43 Prague 2, Czechia.
Center of Biological Defense, Military Health Institute, Military Medical Agency, 561 66 Těchonín, Czechia.
J Control Release. 2020 May 10;321:312-323. doi: 10.1016/j.jconrel.2020.02.026. Epub 2020 Feb 14.
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.
结核病是一个全球性的主要健康问题，需要改进治疗方法，以缩短治疗过程并对抗耐药菌株的出现。开发有效和安全的基于纳米珠的干预措施对于增加感染部位的抗结核药物浓度和降低全身循环中的浓度特别重要，从而避免非靶标毒性作用。在这项工作中，利福平作为一线抗结核药物被包裹在生物相容性和可生物降解的聚酯纳米颗粒中。在已建立的 BALB/c 小鼠肺结核模型中，纳米颗粒改善了药代动力学和药效学。纳米颗粒耐受性良好，比等量的游离利福平效率更高。
