The increase in new cases of drug resistance to first-line drugs such as ethambutol (ETB) makes it necessary to develop improvements for antituberculosis drugs. A new method for improving the bioavailability of active pharmaceutical ingredient (API) was investigated for preventing drug resistance and side-effects of antituberculosis drugs. In this study, an antituberculosis drug delivery system using β-cyclodextrin (β-CD) as the supramolecular carrier of ETB was prepared using the kneading method. The inclusion behaviour of β-CD/ETB inclusion complex in solid and liquid state was investigated. The inclusion complex was characterized using Fourier transform infrared spectroscopy, thermogravimetric analysis, nuclear magnetic resonance (NMR) spectroscopy, and UV-visible spectroscopy. The 1H and nuclear Overhauser effect spectroscopy NMR results indicated the hydrophobic interaction between β-CD and ETB. Meanwhile, the Benesi-Hildebrand equation was used to calculate the formation constant (K) of β-CD/ETB complex in natural condition, pH4, and pH9, which were 105.43, 107.06, and 119.11, respectively. The stoichiometry ratio of β-CD/ETB complex was proven to be 1:1.
Keywords: ethambutol; inclusion complex; tuberculosis drug; β-cyclodextrin.
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