Synthesis, characterization, and in vitro evaluation of gamma radiation-induced PEGylated isoniazid
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Keywords

Antituberculotic
Asparaginase
Humans
Isoniazid
Mycobacterium tuberculosis
Poly(ethylene glycol)
Polymers
Prodrug
Raman
Tuberculosis
UV/Vis

How to Cite

1.
González Torres M, Guzmán-Beltrán S, Mata-Gómez MA, González-Valdez J, Leyva-Gómez G, Melgarejo-Ramírez Y, Brostow W, Velasquillo C, Zúñiga-Ramos J, Rodríguez-Talavera R. Synthesis, characterization, and in vitro evaluation of gamma radiation-induced PEGylated isoniazid. Electron. J. Biotechnol. [Internet]. 2019 Sep. 24 [cited 2024 Dec. 3];41. Available from: https://www.ejbiotechnology.info/index.php/ejbiotechnology/article/view/2019.07.005

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 PEG-INH) 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 PEG-INH 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.

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