PMID- 30632978 OWN - NLM STAT- MEDLINE DCOM- 20190513 LR - 20190513 IS - 2310-6972 (Print) IS - 2310-6905 (Linking) VI - 64 IP - 6 DP - 2018 Nov TI - [Increase of antituberculosis efficiency of rifampicin embedded into phospholipid nanoparticles with sodium oleate]. PG - 505-510 LID - 10.18097/PBMC20186406505 [doi] AB - 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. FAU - Sanzhakov, M A AU - Sanzhakov MA AD - Institute of Biomedical Chemistry, Moscow, Russia. FAU - Ipatova, O M AU - Ipatova OM AD - Institute of Biomedical Chemistry, Moscow, Russia. FAU - Torkhovskaya, T I AU - Torkhovskaya TI AD - Institute of Biomedical Chemistry, Moscow, Russia; Scientific Research Institute of Physical-Chemical Medicine, Moscow, Russia. FAU - Tikhonova, E G AU - Tikhonova EG AD - Institute of Biomedical Chemistry, Moscow, Russia; PLC "IBMH-EcoBioPharm", Moscow, Russia. FAU - Medvedeva, N V AU - Medvedeva NV AD - Institute of Biomedical Chemistry, Moscow, Russia. FAU - Zakharova, T S AU - Zakharova TS AD - Institute of Biomedical Chemistry, Moscow, Russia. FAU - Prozorovskiy, V N AU - Prozorovskiy VN AD - Institute of Biomedical Chemistry, Moscow, Russia. LA - rus PT - Journal Article TT - Povyshenie protivotuberkuleznogo deistviia rifampitsina pri vstraivanii v fosfolipidnye nanochastitsy c oleatom natriia. PL - Russia (Federation) TA - Biomed Khim JT - Biomeditsinskaia khimiia JID - 101196966 RN - 0 (Antitubercular Agents) RN - 0 (Drug Carriers) RN - 2UMI9U37CP (Oleic Acid) RN - 399SL044HN (osteum) RN - VJT6J7R4TR (Rifampin) SB - IM MH - Animals MH - Antitubercular Agents/*pharmacology MH - *Drug Carriers MH - Mice MH - Mycobacterium tuberculosis/drug effects MH - *Nanoparticles MH - *Oleic Acid MH - Rifampin/*pharmacology OTO - NOTNLM OT - CUF OT - M. tuberculosis OT - antituberculosis therapy OT - cell growth OT - phospholipid nanoparticles OT - rifampicin EDAT- 2019/01/12 06:00 MHDA- 2019/05/14 06:00 CRDT- 2019/01/12 06:00 PHST- 2019/01/12 06:00 [entrez] PHST- 2019/01/12 06:00 [pubmed] PHST- 2019/05/14 06:00 [medline] AID - 10.18097/PBMC20186406505 [doi] PST - ppublish SO - Biomed Khim. 2018 Nov;64(6):505-510. doi: 10.18097/PBMC20186406505.