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

• Main Authors: Filipa Santos, Luís C. Branco, Ana Rita C. Duarte
• Format: Article
• Language: English
• Published: MDPI AG 2020-10-01
• Series: Pharmaceutics
• Subjects: ionic liquids & organic salts; tuberculosis; isoniazid; bioavailability; cytotoxicity
• Online Access: https://www.mdpi.com/1999-4923/12/10/952

Tuberculosis is one of the ten causes of morbidity and mortality worldwide caused by <i>Mycobacterium tuberculosis </i>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.