Four different kinds of Lipid Nanoparticles (LNP) encapsulating bedaquiline have been tested in order to evaluate the possibility to decrease adverse effects of this very efficient and recent antibiotic. The parameters that are studied among these different types of LNP are the surface charge as well as targeting of macrophages through trimannose groups grafted to the surface. It was found that these nanocarriers could encapsulate bedaquiline with a very high loading efficiency, exhibited a very good colloidal stability in storage conditions as well as in biological media, and an excellent compatibility with animal cells. Finally, first in vivo evaluation showed that these carriers are able to accumulate strongly in the lungs and that the almost neutral ones without targeting ligands could be the best candidate for tuberculosis treatment.
展开▼