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Open Access Interaction of neomycin, tobramycin and amikacin with melanin in vitro in relation to aminoglycosides-induced ototoxicity

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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

Affiliations: 1: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Medical University of Silesia, Jagiellońska 4, Sosnowiec, PL-41-200, Poland, Email: [email protected] 2: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Medical University of Silesia, Sosnowiec, Poland

Publication date: 2007-03-01

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  • Pharmazie is a leading journal in the field of pharmaceutical sciences. As a peer-reviewed scientific journal, Pharmazie is regularly indexed in the relevant databases like Web of science, Journal Citation Reports and many others. The journal is open for submissions from the whole spectrum of pharnaceutical sciences including Pharmaceutical Chemistry, Experimental and Clinical Pharmacology, Drug Analysis, Pharmaceutics, Pharmaceutical Biology, Clinical Pharmacy etc.
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