Increase of antituberculosis efficiency of rifampicin embedded into phospholipid nanoparticles with sodium oleate

   
Sanzhakov M.A.1, Ipatova O.M.1, Torkhovskaya T.I.2 , Tikhonova E.G.3, Medvedeva N.V.1, Zakharova T.S.1, Prozorovskiy V.N.1

1. Institute of Biomedical Chemistry, Moscow, Russia
2. Institute of Biomedical Chemistry, Moscow, Russia; Scientific Research Institute of Physical-Chemical Medicine, Moscow, Russia
3. Institute of Biomedical Chemistry, Moscow, Russia; PLC “IBMH-EcoBioPharm”, Moscow, Russia
Section: Experimental Study
DOI: 10.18097/PBMC20186406505      PubMed Id: 30632978
Year: 2018  Volume: 64  Issue: 6  Pages: 505-510
The formulation of the antituberculosis drug rifampicin embedded into 20-30 nm nanoparticles from soy phosphatidylcholine and sodium oleate, is characterized by greater bioavailability as compared with free drug substance. In this study higher antituberculosis activity of this formulation was shown. Rifampicin in nanoparticles demonstrated more effective inhibition of M. tuberculosis H37Rv growth: minimal inhibiting concentration (MIC) was twice smaller than for free rifampicin. Administration of this preparation to mice with tuberculosis induced by M. tuberculosis Erdman revealed that after 6 weeks of oral administration the CUF value in lung was 22 times smaller for rifampicin in nanoparticles than for free drug (1.7 un. vs. 37.4 un.). The LD50 value in mice was two fold higher for rifampicin in nanoformulation.
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Keywords: phospholipid nanoparticles, rifampicin, antituberculosis therapy, M. tuberculosis, cell growth, CUF
Citation:

Sanzhakov, M. A., Ipatova, O. M., Torkhovskaya, T. I., Tikhonova, E. G., Medvedeva, N. V., Zakharova, T. S., Prozorovskiy, V. N. (2018). Increase of antituberculosis efficiency of rifampicin embedded into phospholipid nanoparticles with sodium oleate. Biomeditsinskaya khimiya, 64(6), 505-510.
This paper is also available as the English translation: 10.1134/S1990750819030077
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