AMIKACIN, KANAMYCIN AND TOBRAMYCIN BINDING TO MELANIN IN THE PRESENCE OF Ca2+ AND Mg2+ IONS

作者：Wrzesniok Dorota; Buszman Ewa^*; Miernik Biela Ewa

来源：Acta Poloniae Pharmaceutica, 2012, 69(6): 1035-1041.

• amikacin
• kanamycin
• tobramycin
• melanin
• drug-melanin complexes

The aim of the presented work was to examine the interaction of amikacin, kanamycin and tobramycin with melanin in the presence of Ca2+ and Mg2+ ions. It has been demonstrated that the analyzed aminoglycosides form complexes with melanin in the presence of metal ions and the amount of drugs bound to the polymer increases with increasing initial antibiotics concentration. It has been also shown that two classes of binding sites participate in the formation of amikacin, kanamycin and tobramycin complexes with melanin containing Ca2+ or Mg2+ ions: high affinity binding sites (n(1)) with the association constant K-1 similar to 10(4)-10(5)M(-1) and low affinity binding sites (n(2)) with K2 similar to 10(3) M-1. It has been demonstrated that calcium and magnesium significantly decrease the number of total binding sites (n(tot)) as compared with aminoglycoside-melanin complexes obtained in the absence of metal ions.

• 出版日期2012-12