resumo
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. © 2019 American Chemical Society.
autores
AndrŽ V.; Da Silva A.R.F.; Fernandes A.; Frade R.; Garcia C.; Rijo P.; Antunes A.M.M.; Rocha J.; Duarte M.T.
nossos autores
João Rocha
Prof. Catedráticoagradecimentos
The authors acknowledge Fundaca_ › para a Cienci‰ e a Tecnologia (FCT, Portugal) (PEst-OE/QUI/UI0100/2013) and FEDER to the project PTDC/QUI-OUT/30988/2017 for funding. We also wish to thank the European Union, QREN, FEDER through Programa Operacional Factores de Com-petitividade (COMPETE), and CICECO_Aveiro Institute of Materials, POCI-01-0145-FEDER-007679 (FCT ref no. UID/ CTM/50011/2013), financed by national funds through the FCT/MEC and when appropriate cofinanced by FEDER under the PT2020 Partnership Agreement. The authors further acknowledge Ms. C. Iolanda Santos for the use of the HPLC.