Numerous antimicrobial drugs have been prescribed to kill or inhibit the growth of microbes such as bacteria, fungi, and viruses. Despite the known therapeutic efficacy of these drugs, inefficient delivery could result in an inadequate therapeutic index and several side effects. In order to overcome this adversity, the present study investigated antibiotic drug loading in zeolitic imidazolate frameworks (ZIFs), in association with ZnO nanoparticles with known antimicrobial properties. In an economic synthesis method, the ZnO surface was first converted to ZIF-8 with 2-methylimidazole as a ligand, resulting in a ZnO@ZIF-8 structure. This system enables the high drug-loading efficiency (46%) of an antimicrobial drug, ciprofloxacin, within the pores of the ZIF-8. This association provides a control of the release of the active moieties, in simulated body-fluid conditions, with a maximum of 67% released in 96 h. The antibacterial activities of ZnO@ZIF-8 and CIP-ZnO@ZIF-8 were tested against the Gram-positive Staphylococcus aureus strain and the Gram-negative Pseudomonas aeruginosa strain, showing good growth inhibition. This result was obtained by combining ZnO@ZIF-8 with ciprofloxacin in a minimal inhibitory concentration (MIC) that was 10 times lower than ZnO@ZIF-8 for S. aureus and 200 times lower for P. aeruginosa, suggesting that CIP-ZnO@ZIF-8 may have potential application in prolonged antimicrobial treatment.
Zinc oxide (ZnO) and iron oxide (IO) nanoparticles have been identified as promising candidates for biomedical applications, based on their unique physicochemical properties. The association of these nanoparticles in a single system creates a bimodal entity, allowing the excellent luminescent properties of ZnO quantum dots to be combined with the contrast agent of IO for magnetic resonance imaging (MRI). The present study focuses on the luminescent and MRI properties of a new poly(lactic-co-glycolic acid) (PLGA) nanocarrier system formulation containing ZnO NPs and IO NPs in different nominal ratios. Microscopic analysis (TEM and SEM) reveals a circular morphology with IO and ZnO NPs. The average diameter of the particles was determined to be 220 nm, as measured by DLS. The luminescence results indicate that the PLGA system shows strong emission in the visible range, and the MRI analysis shows a high r2 relaxivity of 171 mM−1 s−1 at 7T. The optimized formulation, exhibiting a molar ratio of Fe:Zn ranging from 1:10 to 1:13 (mol:mol), demonstrates superior fluorescence and MRI performance, underscoring the significance of nanoparticle composition in bimodal imaging applications. The systems evaluated demonstrate no toxicity in the THP-1 cells for doses of up to 128 µg mL−1, with efficient labeling after 4 h of incubation, yielding images of strong luminescence and T2 contrast. The PLGA:ZnO:IO system demonstrates considerable potential as a bimodal platform for diagnostic imaging.
Background: A drug with poor water-solubility, like Dexamethasone acetate, can present lower bioavailability conventional for pharmaceutical formulations, and the presence of polymorphs in the raw material can lead to drug quality problems. Objective: In this study, nanocrystals of dexamethasone acetate were synthesized by high pressure homogenizer (HPH) method in surfactant poloxamer 188 (P188) solid dispersion and the bioavailable in raw material with polymorphism presence was evaluated. Methods: The powder pre-suspension was prepared by the HPH process, and the nanoparticles formed were incorporated in P188 solutions. The nanocrystals formed were characterized by techniques of XRD, SEM, FTIR, thermal analysis by differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA), dynamic light scattering (DLS) to analyze the particle size and zeta potential, and in vitro evaluation by dissolution studies. Results: The characterization techniques were adequate to show the presence of raw material with physical moisture between two dexamethasone acetate polymorphs. The nanocrystals formed in the presence of the P188 in the formulation showed a considerable increase in the rate of dissolution of the drug in the medium and in the size of the stable nanocrystals, even in the presence of dexamethasone acetate polymorphs. Conclusion: The results showed that it was possible to produce dexamethasone nanocrystals by HPH process with regular size by the presence of the small amount of P188 surfactant. This article presents a novelty in the development of dexamethasone nanoparticles that have different polymorphic forms in their physical composition.