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.
β-cyclodextrin, tuberculosis drug, ethambutol, inclusion complex
GOH, SOEN QENG; CHAN, QIAO HUI; ADNAN, ROHANA; and RAHIM, NURUL YANI
"Preparation and characterisation of ethambutol with β-cyclodextrin: a comprehensive molecular insight into host-guest interaction,"
Turkish Journal of Chemistry: Vol. 46:
6, Article 16.
Available at: https://journals.tubitak.gov.tr/chem/vol46/iss6/16