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Novel Antibacterial Azelaic Acid BioMOFs
journal contribution
posted on 2019-12-05, 19:05 authored by Silvia Quaresma, Vânia André, Alexandra M. M. Antunes, Sérgio M.
F. Vilela, Georgiana Amariei, Ana Arenas-Vivo, Roberto Rosal, Patricia Horcajada, M. Teresa DuarteThe development of metal–organic frameworks (MOFs)
for bioapplications
has gained great relevance over the last few years, mainly due to
their potential as drug carriers and/or imaging agents. Although the
bioactive azelaic acid has also been widely used as an antibacterial
and anti-inflammatory drug, it presents low solubility, so of utmost
importance is the development of more soluble formulations with sustained
activity. In this contribution, we prove that new azelaic acid-based
metal biomolecule frameworks (BioMOFs) are a viable pathway to achieve
this goal. Therefore, five novel MOFs were prepared by a simple, low-cost,
and environmentally friendly mechanochemical approach, combining azelaic
acid with endogenous cations (i.e., K+, Na+,
and Mg2+): [K2(H2AZE)(AZE)] (1), [Na4(HAZE)4] (2), [Na2(AZE)(H2O)] (3), and two different
polymorphic forms of [Mg(AZE)(H2O)3] (4) and (5) (where H2AZE - neutral
azelaic acid; HAZE - mono-deprotonated azelaic acid; AZE - di-deprotonated
azelaic acid). After full structural characterization using single-crystal
X-ray diffraction data and other complementary standard solid-state
techniques, their thermal and moisture stabilities as well as aqueous
solubility were assessed. Finally, their antibacterial activity was
evaluated against two Gram-positive bacteria (Staphylococcus
aureus and Staphylococcus epidermidis),
commonly present on the skin. All MOF materials exhibit good stability
and higher solubility than azelaic acid. In addition, BioMOF 1 has shown good antibacterial activity both at pH 5 and 6.5.
Thus, 1 has shown to be a promising candidate to further
develop new topical formulations of H2AZE.