Результаты исследований: Вклад в журнал › Статья › Рецензирование
Результаты исследований: Вклад в журнал › Статья › Рецензирование
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TY - JOUR
T1 - Optimization, characterization, and cytotoxicity studies of novel anti-tubercular agent-loaded liposomal vesicles
AU - Obiedallah, Manar
AU - Mironov, Maxim
AU - Belyaev, Danila
AU - Ene, Antoaneta
AU - Vakhrusheva, Diana
AU - Krasnoborova, Svetlana Yu.
AU - Bershitsky, Sergey
AU - Shchepkin, Daniil
AU - Minin, Artem
AU - Ishmetova, Rashida
AU - Ignatenko, Nina
AU - Tolshchina, Svetlana
AU - Fedorova, Olga
AU - Rusinov, Gennady l.
N1 - This research was funded by the Ministry of Science and Higher Education of the Russian Federation (Agreement on the provision of grants from the federal budget in the form of subsidies under paragraph 4 of Article 78.1 of the Budget Code of the Russian Federation, Moscow, 1 October 2020 No. 075-15-2020-777). Manar M. Obiedallah would like to acknowledge the partial financial support provided by the Egyptian Ministry of Higher Education and Scientific Research. The work of author AE was supported by Dunarea de Jos University of Galati, Romania.
PY - 2024
Y1 - 2024
N2 - The treatment of tuberculosis is still a challenging process due to the widespread of pathogen strains resistant to antibacterial drugs, as well as the undesirable effects of anti-tuberculosis therapy. Hence, the development of safe and effective new anti-antitubercular agents, in addition to suitable nanocarrier systems, has become of utmost importance and necessity. Our research aims to develop liposomal vesicles that contain newly synthesized compounds with antimycobacterial action. The compound being studied is a derivative of imidazo-tetrazine named 3-(3,5-dimethylpyrazole-1-yl)-6-(isopropylthio) imidazo [1,2-b] [1,2,4,5] tetrazine compound. Several factors that affect liposomal characteristics were studied. The maximum encapsulation efficiency was 53.62 ± 0.09. The selected liposomal formulation T8* possessed a mean particle size of about 205.3 ± 3.94 nm with PDI 0.282, and zeta potential was + 36.37 ± 0.49 mv. The results of the in vitro release study indicated that the solubility of compound I was increased by its incorporation in liposomes. The free compound and liposomal preparation showed antimycobacterial activity against Mycobacterium tuberculosis H37Rv (ATCC 27294) at MIC value 0.94–1.88 μg/ml. We predict that the liposomes may be a good candidate for delivering new antitubercular drugs.
AB - The treatment of tuberculosis is still a challenging process due to the widespread of pathogen strains resistant to antibacterial drugs, as well as the undesirable effects of anti-tuberculosis therapy. Hence, the development of safe and effective new anti-antitubercular agents, in addition to suitable nanocarrier systems, has become of utmost importance and necessity. Our research aims to develop liposomal vesicles that contain newly synthesized compounds with antimycobacterial action. The compound being studied is a derivative of imidazo-tetrazine named 3-(3,5-dimethylpyrazole-1-yl)-6-(isopropylthio) imidazo [1,2-b] [1,2,4,5] tetrazine compound. Several factors that affect liposomal characteristics were studied. The maximum encapsulation efficiency was 53.62 ± 0.09. The selected liposomal formulation T8* possessed a mean particle size of about 205.3 ± 3.94 nm with PDI 0.282, and zeta potential was + 36.37 ± 0.49 mv. The results of the in vitro release study indicated that the solubility of compound I was increased by its incorporation in liposomes. The free compound and liposomal preparation showed antimycobacterial activity against Mycobacterium tuberculosis H37Rv (ATCC 27294) at MIC value 0.94–1.88 μg/ml. We predict that the liposomes may be a good candidate for delivering new antitubercular drugs.
UR - http://www.scopus.com/inward/record.url?partnerID=8YFLogxK&scp=85181455194
UR - https://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=tsmetrics&SrcApp=tsm_test&DestApp=WOS_CPL&DestLinkType=FullRecord&KeyUT=001136960700001
U2 - 10.1038/s41598-023-49576-2
DO - 10.1038/s41598-023-49576-2
M3 - Article
VL - 14
JO - Scientific Reports
JF - Scientific Reports
SN - 2045-2322
IS - 1
M1 - 524
ER -
ID: 51655727