Mg- and Mn-MOFs Boost the Antibiotic Activity of Nalidixic Acid

Abstract

The development of metal-organic frameworks (MOFs) enclosing active pharmaceutical ingredients is of considerable interest, as their use in controlled drug release and delivery is very promising. Although nalidixic acid is an antibiotic with a broad spectrum of biological applications, effective mainly against Gram-negative infections, its oral bioavailability is low due to a poor solubility and slow dissolution. Herein, we report new metal-organic frameworks (BioMOFs) comprising nalidixic acid and divalent magnesium and manganese ions. These compounds showed an adequate cytotoxicity and improved antimicrobial activity, especially against Gram-negative bacteria. These BioMOFS are among the first examples containing active pharmaceutical ingredients as linkers. Importantly, it is shown that a remarkable increase of the antimicrobial activity of certain antibiotics may be achieved by delivering them in the form of BioMOFs.

Keywords: antibiotics; antimicrobial activity; mechanochemistry; metal−organic frameworks; nalidixic acid.