BIODISTRIBUTION OF RIFABUTIN POLYMERIC TRANSPORT FORM

Cover Page
  • Authors: Kuznetsova I.G.1, Dubovik E.G.2, Dubovik N.S.1, Komarov T.N.1, Medvedev Y.V.1, Men'shchikova L.A.1, Severin S.E.1, Shokhin I.E.1, Yarushok T.A.1
  • Affiliations:
    1. Sechenov First Moscow State Medical University, Moscow, Russian Federation
    2. Lomonosov Moscow State University, Moscow, Russian Federation
  • Issue: Vol 70, No 3 (2015)
  • Pages: 366–371
  • Section: SHORT MESSAGES
  • URL: https://vestnikramn.spr-journal.ru/jour/article/view/44
  • DOI: https://doi.org/10.15690/vramn.v70i3.1335

Abstract


Background: One way to increase drug efficacy is to provide a drug delivery transport system to the target organ. A widely used method is to incorporate the drug in a biodegradable polymer composition with forming nanosized drug’s transport forms. Objective: Our aim was to investigate the tissue biodistribution of antibiotic rifabutin transport system based on lactic and glycolic acids copolymer, and to compare it with the pure substance of rifabutin. Methods: These substances were administered to two groups of rats intragastrically in the doses of 10 mg/kg. After a certain period of time, the animals were sacrificed by cervical dislocation. Samples preparation for analysis was carried out of the liquid-liquid extraction. Active substance’s concentrations were measured by high performance liquid chromatography method. Results: The study included 8-week-aged Wistar rats of both sexes weighing 0.22±0.02 kg. Animals were divided into 2 groups. The study group received polymer form of antibiotic, and the comparison group received substance of rifabutin. In intervals of 10 min, 30 min, 1 h, 2 h, 4 h, 7 h, 15 h, 24 h after drug administration liver, lung, spleen, kidney, intestines, stomach, heart and brain were resected respectively. Organs were measured by their weight. The drug was not detected in the brain. Rifabutin was determined in other examined tissues within 10 minutes and the maximum drug concentration in organs was fixed in 1.5–3.5 hours after administration. The rifabutin concentrations defined in the lungs were significantly higher in polymer form (p <0.05). The polymer form’s distribution coefficient was higher in the liver and lungs (15.83 and 10.14 μg/g respectively) in comparison with the substance one. The minimum amount of the active ingredient was observed in the heart (0.02 μg/g). Conclusion: It is shown that the inclusion of the drug in a polymeric form substantially alters its localization in organs and tissues. Extensive biodistribution nanorifabutin in lung tissue, liver and spleen is established.

 

 


I. G. Kuznetsova

Sechenov First Moscow State Medical University, Moscow, Russian Federation

Author for correspondence.
Email: irina1105@rambler.ru

Russian Federation

старший преподаватель кафедры биологической химии лечебного факультета Первого МГМУ им. И.М. Сеченова
Адрес: 119048, Москва, ул. Трубецкая, д. 8, стр. 2, тел.: +7 (495) 609-14-00, доб. 3145

E. G. Dubovik

Lomonosov Moscow State University, Moscow, Russian Federation

Email: dubovik@mail.ru

Russian Federation

аспирант кафедры биоинженерии биологического факультета МГУ им. М.В. Ломоносова
Адрес: 119234, Москва, Ленинские горы, д. 1, тел.: +7 (495) 939-10-00, доб. 2401

N. S. Dubovik

Sechenov First Moscow State Medical University, Moscow, Russian Federation

Email: berezanatawa@yandex.ru

Russian Federation

кандидат фармацевтических наук, ассистент кафедры фармацевтической химии фармацевтического факультета Первого МГМУ им. И.М. Сеченова
Адрес: 119048, Москва, ул. Трубецкая, д. 8, стр. 2, тел.: +7 (495) 609-14-00, доб. 1636

T. N. Komarov

Sechenov First Moscow State Medical University, Moscow, Russian Federation

Email: t.n.komarov@yandex.ru

Russian Federation

кандидат фармацевтических наук, ассистент кафедры фармацевтической химии
фармацевтического факультета Первого МГМУ им. И.М. Сеченова
Адрес: 119048, Москва, ул. Трубецкая, д. 8, стр. 2, тел.: +7 (495) 128-57-00

Yu. V. Medvedev

Sechenov First Moscow State Medical University, Moscow, Russian Federation

Email: y125195@yandex.ru

Russian Federation

кандидат фармацевтических наук, старший преподаватель кафедры
фармацевтической химии фармацевтического факультета Первого МГМУ им. И.М. Сеченова
Адрес: 119048, Москва, ул. Трубецкая, д. 8, стр. 2, тел.: +7 (495) 128-57-00

L. A. Men'shchikova

Sechenov First Moscow State Medical University, Moscow, Russian Federation

Email: lily-chka@mail.ru

Russian Federation

аспирант кафедры фармацевтической химии фармацевтического факультета Первого МГМУ им. И.М. Сеченова
Адрес: 119048, Москва, ул. Трубецкая, д. 8, стр. 2, тел.: +7 (495) 128-57-00

S. E. Severin

Sechenov First Moscow State Medical University, Moscow, Russian Federation

Email: sergsev@inbox.ru

Russian Federation

член-корреспондент РАН, профессор, заведующий кафедрой биологической химии
лечебного факультета Первого МГМУ им. И.М. Сеченова
Адрес: 119048, Москва, ул. Трубецкая, д. 8, стр. 2, тел.: +7 (499) 613-23-20

I. E. Shokhin

Sechenov First Moscow State Medical University, Moscow, Russian Federation

Email: sovdep2007@yandex.ru

Russian Federation

кандидат фармацевтических наук, старший преподаватель кафедры фармацевтической химии фармацевтического факультета Первого МГМУ им. И.М. Сеченова
Адрес: 119048, Москва, ул. Трубецкая, д. 8, стр. 2, тел.: +7 (495) 128-57-00

T. A. Yarushok

Sechenov First Moscow State Medical University, Moscow, Russian Federation

Email: doctormarmalade@mail.ru

Russian Federation

кандидат фармацевтических наук, ассистент кафедры фармацевтической химии
фармацевтического факультета Первого МГМУ им. И.М. Сеченова
Адрес: 119048, Москва, ул. Трубецкая, д. 8, стр. 2, тел.: +7 (495) 128-57-00

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