Efficacy of an Intravenous Form of Rifapentine in a Model of Experimental Tuberculosis in Mice
- 作者: Ostrovskii K.1, Osipova N.1, Vanchugova L.1, Shipulo E.1, Potapov V.2, Pereverzeva É.3, Treshchalin I.3, Maksimenko O.1, Gel’perina S.1
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隶属关系:
- Nanosistema Scientific Industrial Complex
- State Scientific Center for Applied Microbiology and Biotechnology
- G. F. Gauze Science Research Institute for the Discovery of New Antibiotics
- 期: 卷 51, 编号 7 (2017)
- 页面: 616-621
- 栏目: Article
- URL: https://journals.rcsi.science/0091-150X/article/view/244732
- DOI: https://doi.org/10.1007/s11094-017-1663-7
- ID: 244732
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Solubilization of rifapentine with human serum albumin (HSA) was used to produce a water-miscible form consisting of a colloidal suspension of particles of size 538 ± 9 nm. Dilution of the suspension more than 20-fold led to dissociation of the aggregates formed during solubilization procedure, producing a transparent solution. This was associated with a reduction in particle size to 10 – 20 nm, corresponding to the particle size in HSA solution at the same concentration. A fluorescence method showed that suspensions contained both free rifapentine and its complex with HSA. Studies of the activity against the pathogen of tuberculosis, Mycobacterium tuberculosis H37Rv, in a model of acute infection in Balb/c mice showed that the water-miscible form of rifapentine given intravenously had high activity against mycobacteria, comparable with the activity of rifapentine substance, decreasing mycobacterial loadings in the parenchymatous organs from 106 – 107 to 102 – 103 cfu/organ. Thus, use of HSA as solubilizer yielded an intravenous form of rifapentine retaining the activity of the antibiotic against Mycobacterium tuberculosis.
作者简介
K. Ostrovskii
Nanosistema Scientific Industrial Complex
编辑信件的主要联系方式.
Email: ostrovkp@mail.ru
俄罗斯联邦, 20 Seventh Kozhukhovskaya Street, Moscow, 115193
N. Osipova
Nanosistema Scientific Industrial Complex
Email: ostrovkp@mail.ru
俄罗斯联邦, 20 Seventh Kozhukhovskaya Street, Moscow, 115193
L. Vanchugova
Nanosistema Scientific Industrial Complex
Email: ostrovkp@mail.ru
俄罗斯联邦, 20 Seventh Kozhukhovskaya Street, Moscow, 115193
E. Shipulo
Nanosistema Scientific Industrial Complex
Email: ostrovkp@mail.ru
俄罗斯联邦, 20 Seventh Kozhukhovskaya Street, Moscow, 115193
V. Potapov
State Scientific Center for Applied Microbiology and Biotechnology
Email: ostrovkp@mail.ru
俄罗斯联邦, Obolensk, Serpukhov District, Moscow Region, 142279
É. Pereverzeva
G. F. Gauze Science Research Institute for the Discovery of New Antibiotics
Email: ostrovkp@mail.ru
俄罗斯联邦, 11 Bol’shaya Pirogovskaya Street, Moscow, 119021
I. Treshchalin
G. F. Gauze Science Research Institute for the Discovery of New Antibiotics
Email: ostrovkp@mail.ru
俄罗斯联邦, 11 Bol’shaya Pirogovskaya Street, Moscow, 119021
O. Maksimenko
Nanosistema Scientific Industrial Complex
Email: ostrovkp@mail.ru
俄罗斯联邦, 20 Seventh Kozhukhovskaya Street, Moscow, 115193
S. Gel’perina
Nanosistema Scientific Industrial Complex
Email: ostrovkp@mail.ru
俄罗斯联邦, 20 Seventh Kozhukhovskaya Street, Moscow, 115193