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The antituberculosis drug bedaquiline is efficiently nanoencapsulated

AutorLucía, A.; Matteis, Laura de; Serrano-Sevilla, Inés; Fuente, Jesús M. de la
Fecha de publicación2017
CitaciónFEMS 2017
Resumen[Backgrounds]: Antibiotic resistance in Mycobacterium tuberculosis is a global health emergency, and rising cases of MDR and XDR-TB are making increasingly difficult to treat tuberculosis. In 2012 the FDA approved the use of bedaquiline, the first drug designed to treat MDR-TB. It is very effective but shows serious side effects, so it can only be prescribed when no other options are available. Novel drug delivery systems based on nanocarriers are a promising strategy to overcome current therapeutic challenges. They improve drug solubility, protect the drugs, and allow a controlled release of the medication. Additionally they can be modified to allow selective transport to the sites of infection. [Objectives]: The development of effective and safe nanotherapy is particularly relevant in the treatment of MDRTB, as it requires very long treatments with highly toxic drugs. Therefore nanoencapsulation of bedaquiline is of special interest. [Methods]: Chitosan based nanocapsules and Lipid NanoParticles, based on the Lipidots® technology, have been synthesized and optimized for the encapsulation of bedaquiline. upon quantification of drug loading efficiency, improvement of the drug payload, and nanoparticles stability amelioration in storage conditions. For the best candidates, drug release has been determined in biological media for in vitro assays. The antimycobacterial activity has been evaluated, and their cytotoxicity has been assayed in different cell lines. [Conclusions]: Bedaquiline has been encapsulated in two different types of carriers, and the final nanoparticles have been totally characterized being found to be fully active as the free drug, and no cytotoxic.
DescripciónResumen del trabajo presentado al 7th Congress of European Microbiologists, celebrado en Valencia (España) del 9 al 13 de julio de 2017.-- et al.
URIhttp://hdl.handle.net/10261/164034
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