Synthesis, characterization, and in vitro evaluation of gamma radiationinduced PEGylated isoniazid
Electron. j. biotechnol
;
41: 81-87, sept. 2019. tab, graf, ilus
Article
in English
| LILACS
| ID: biblio-1087242
ABSTRACT
Background:
The search for innovative anti-tubercular agents has received increasing attention in tuberculosis chemotherapy because Mycobacterium tuberculosis infection has steadily increased over the years. This underlines the necessity for new methods of preparation for polymer-drug adducts to treat this important infectious disease. The use of poly(ethylene glycol)(PEG) is an alternative producing anti-tubercular derivatives. However, it is not yet known whether PEGylated isonicotinylhydrazide conjugates obtained by direct links with PEG are useful for therapeutic applications.Results:
Here, we synthesized a PEGylated isoniazid (PEG-g-INH or PEGINH) by gamma radiation-induced polymerization, for the first time. The new prodrugs were characterized using Raman and UV/Vis spectrometry. The mechanism of PEGylated INH synthesis was proposed. The in vitro evaluation of a PEGylated isonicotinylhydrazide macromolecular prodrug was also carried out. The results indicated that PEGINH inhibited the bacterial growth above 95% as compared with INH, which showed a lower value (80%) at a concentration of 0.25 µM. Similar trends are observed for 0.1, 1, and 5 µM.Conclusions:
In summary, the research suggests that it is possible to covalently attach the PEG onto INH by the proposed method and to obtain a slow-acting isoniazid derivative with little toxicity in vitro and higher antimycobacterial potency than the neat drug.
Full text:
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Index:
LILACS (Americas)
Main subject:
Polyethylene Glycols
/
Isoniazid
/
Mycobacterium tuberculosis
/
Antitubercular Agents
Language:
English
Journal:
Electron. j. biotechnol
Journal subject:
Biotechnology
Year:
2019
Type:
Article
Affiliation country:
Mexico
/
United States
Institution/Affiliation country:
Instituto Nacional de Enfermedades Respiratorias Ismael Cosío Villegas/MX
/
Instituto Nacional de Rehabilitación "Luís Guillermo Ibarra Ibarra"/MX
/
School of Engineering and Science/MX
/
Universidad Nacional Autónoma de Mexico/MX
/
Universidad Nacional Autónoma de México/MX
/
University of North Texas/US
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