Dexamethasone Acetate Nanocrystals, Characterization and Dissolution Studies in Presence of Polymorphic Phases.

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.

ZnO@ZIF-8 Nanoparticles as Nanocarrier of Ciprofloxacin for Antimicrobial Activity.

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.

Sustainable Antibacterial Activity of Polyamide Fabrics Containing ZnO Nanoparticles.

In this study, we present an unprecedented study on the influence of parameters such as dyeing, softening, and number of washes on the maintenance of the antibacterial activity of polyamide fabrics containing zinc oxide nanoparticles (ZnO NPs) impregnated by a simple and easy-to-scale technique. ZnO NPs were synthesized by the sol-gel method at different reaction times (1, 3, and 24 h), followed by surface modification with (3-glycidyloxypropyl)trimethoxysilane (GPTMS) and water dispersion. The reaction times of ZnO NP synthesis were modified to evaluate their influence on particle size and antibacterial activity after impregnation in fabrics. The presence of ZnO NPs in fabrics was observed by different techniques such as X-ray diffraction, infrared vibrational spectroscopy, scanning electron microscopy, and energy-dispersive X-ray spectroscopy. The mean diameter values of the ZnO NPs calculated in this work from different techniques remained at 5 nm regardless of the reaction time revealing the efficient control of the nanoparticle size, important for desired applications as ZnO NPs smaller than 10 nm show improved antibacterial activity. The antibacterial activity of fabrics containing ZnO NPs indicated that polyamide fabrics after impregnation with ZnO NPs synthetized have great and similar biocidal potential against Staphylococcus aureus and Escherichia coli both with and without the presence of a fabric softener or a dye. The antibacterial behavior of the different polyamide fabrics remained after 10 and 20 washing cycles. The results shown in this study demonstrated the possibility of obtaining polyamide fabrics containing ZnO NPs with the antibacterial activity resistant to chemical treatments used by industries as a softener or a dye. The results also reveal the maintenance of the antimicrobial activity of fabrics after several washing cycles. The reaction time of 1 for the production of ZnO NPs and the versatility of polyamide fabrics allow their application in different environments to control microbial infections.