Abstract
Metal ions play a key role in living systems and are used to perform different physiological activities in our body. Complexation of drugs with metal ions is known to influence the bioavailability and other pharmacokinetic properties of drugs. In the present work, complexation of two essential cations, Mg 2+ and Ca 2+ with zidovudine (AZT), the first approved antiretroviral drug for human immunodeficiency virus (HIV) has been studied by conductometry and spectrophotometry. The plots of molar conductance versus the mole ratio of [AZT]/[M 2+ ], Job’s method of continuous variation and mole ratio method showed the stoichiometry to be 1:1 (M 2+ :AZT) for both the cations. The metal ion-AZT complexes formed through the nitrogen of the azide group were further ascertained by liquid chromatography-mass spectrometric analysis. The formation constants of the complexes as evaluated by the conductance method and the Rose-Drago method were in good agreement. The values of thermodynamic parameters (∆H and ∆S) for the formation of complexes were obtained from the Van’t Hoff plots. The results revealed that both the complexation reactions were spontaneous, endothermic and entropy stabilized. KEY WORDS : Zidovudine, Conductometry, Spectrophotometry, Liquid chromatography-mass spectrometry, Formation constant, Thermodynamic parameters Bull. Chem. Soc. Ethiop. 2017 , 31(3), 423-433. DOI: http://dx.doi.org/10.4314/bcse.v31i3.6
Highlights
The complexation study of biologically important medicinal agents or drug molecules with different metal ions found in body fluids has become an important area of research in drug design and development
Electron rich drug molecules combine with metal ions to give “metal-based drugs” or “elemental medicines”, having unique therapeutic applications [2,3,4]
As part of our on-going research into drug-metal ion interaction study, in the present work we report Mg2+ and Ca2+ binding with AZT using two simple and versatile techniques like spectrophotometry and conductometry [26]
Summary
The complexation study of biologically important medicinal agents or drug molecules with different metal ions found in body fluids has become an important area of research in drug design and development. As part of our on-going research into drug-metal ion interaction study, in the present work we report Mg2+ and Ca2+ binding with AZT using two simple and versatile techniques like spectrophotometry and conductometry [26]. Molar ratio method [28] and Job’s method of continuous variation [29] were used to determine the stoichiometry of metal ion-AZT complexes.
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