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Article

Organic Salts Based on Isoniazid Drug: Synthesis, Bioavailability and Cytotoxicity Studies

LAQV, REQUIMTE, Departamento de Química da Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa, 2829-516 Caparica, Portugal
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Pharmaceutics 2020, 12(10), 952; https://doi.org/10.3390/pharmaceutics12100952
Received: 7 August 2020 / Revised: 28 September 2020 / Accepted: 30 September 2020 / Published: 10 October 2020
(This article belongs to the Section Drug Targeting and Design)
Tuberculosis is one of the ten causes of morbidity and mortality worldwide caused by Mycobacterium tuberculosis complex. Some of the anti-tuberculosis drugs used in clinic studies, despite being effective for the treatment of tuberculosis, present serious adverse effects as well as poor bioavailability, stability, and drug-resistance problems. Thus, it is important to develop approaches that could provide shorter drug regimens, preventing drug resistance, toxicity of the antibiotics, and improve their bioavailability. Herein, we reported the use of organic salts based on the isoniazid drug, which can act as an organic cation combined with suitable organic anions such as alkylsulfonate-based (mesylate, R or S-Camphorsulfonate), carboxylate-based (glycolate, vanylate) and sacharinate. The synthesis, characterization, and cytotoxicity studies comparing with the original isoniazid drug have been performed. The possibility to explore dicationic salts seems promising in order to improve original bioavailability, and promote the elimination of polymorphic forms as well as higher stability, which are relevant characteristics that the pharmaceutical industry pursues. View Full-Text
Keywords: ionic liquids & organic salts; tuberculosis; isoniazid; bioavailability; cytotoxicity ionic liquids & organic salts; tuberculosis; isoniazid; bioavailability; cytotoxicity
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MDPI and ACS Style

Santos, F.; Branco, L.C.; Duarte, A.R.C. Organic Salts Based on Isoniazid Drug: Synthesis, Bioavailability and Cytotoxicity Studies. Pharmaceutics 2020, 12, 952. https://doi.org/10.3390/pharmaceutics12100952

AMA Style

Santos F, Branco LC, Duarte ARC. Organic Salts Based on Isoniazid Drug: Synthesis, Bioavailability and Cytotoxicity Studies. Pharmaceutics. 2020; 12(10):952. https://doi.org/10.3390/pharmaceutics12100952

Chicago/Turabian Style

Santos, Filipa, Luís C. Branco, and Ana R.C. Duarte 2020. "Organic Salts Based on Isoniazid Drug: Synthesis, Bioavailability and Cytotoxicity Studies" Pharmaceutics 12, no. 10: 952. https://doi.org/10.3390/pharmaceutics12100952

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