in vitro in relation to aminoglycosides-induced ototoxicity
Interaction of neomycin, tobramycin and amikacin with melanin
The aim of this study was to examine in vitro the interaction between aminoglycoside antibiotics displaying adverse ototoxic effects and melanin which is a constituent of the inner ear. The binding of neomycin, tobramycin and amikacin to model synthetic melanin was studied. It
has been demonstrated that all the investigated aminoglycosides form stable complexes with melanin biopolymer. The obtained results show that the amount of drug bound to melanin increases with the increase of initial drug concentration and the incubation time. An analysis of drugs binding
to melanin by the use of Scatchard plots has shown that at least two classes of independent binding sites must be implicated in the studied aminoglycoside antibiotic-melanin complexes formation: strong binding sites (n1) with the association constant K1 ∼ 0.2–2.0
· 105 M–1 and weak binding sites (n2) with K2 ∼ 1.0–4.9 · 103 M–1. Based on the values of association constants the following order of drugs affinity to DOPA-melanin was found: tobramycin
> amikacin ≫ neomycin. The ability of the analyzed aminoglycoside antibiotics to form complexes with melanin in vitro may be one of the reasons for their ototoxicity in vivo, as a result of their accumulation in melanin in the inner ear.
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Document Type: Research Article
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Medical University of Silesia, Jagiellońska 4, Sosnowiec, PL-41-200, Poland, Email: [email protected]
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Medical University of Silesia, Sosnowiec, Poland
Publication date: 2007-03-01
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