The 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.