Abstract
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.
Highlights
The pharmaceutical industry and research community are continuously trying to improve their approaches and redesign drugs to enhance their therapeutic efficiency, while at the same time reducing the waste produced in the research and manufacture of drugs
In the synthesis of isoniazid based on organic salts and ionic liquids (API-OSILs), the isoniazid drug was used as organic cation and different counterions were selected
All obtained active pharmaceutical ingredients (APIs)-OSILs were characterized by 1H and 13C NMR, FTIR, and elemental analysis in order to prove the desired organic chemical structure as well as final purities
Summary
The pharmaceutical industry and research community are continuously trying to improve their approaches and redesign drugs to enhance their therapeutic efficiency, while at the same time reducing the waste produced in the research and manufacture of drugs. The use of organic salts and ionic liquids (OSILs) for therapeutic applications has been explored, using an API in its ionic form (e.g., ampicillin, [9,10,11] zoledronic acid [12], and ibuprofen [13]) and combining it with biocompatible counterions, producing API-OSILs. The use of API-OSILs allows the design of improved drugs that may modify the functionality and can provide important characteristics to the original API [6,14,15]. The use of API-OSILs allows the design of improved drugs that may modify the functionality and can provide important characteristics to the original API [6,14,15] These API-OSILs present higher stability, solubility, dissolution rate and permeability when compared to the pure drug itself, counterions added to the API could confer some potential toxicity that may lead to dose adjustments and more specific tests for the safety evaluation of these API-OSILs should be required [6]
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