The search for alternative antimicrobial agents is attracting increasing scientific interest. Natural products of plant origin are sources of several substances with proven biological activities, including antimicrobial activity. The encapsulation of these products in the form of a nanoemulsion seeks to overcome problems inherent to these products, such as instability and degradation. Based on these considerations, we carried out a bibliographical survey of nanoemulsions produced from plant-derived substances, such as essential oils and extracts, with antimicrobial potential, focusing on antibacterial, antifungal and antiviral activities. Articles and documents published in scientifically relevant journals, as well as keywords classified from Health Sciences Descriptors, were used. All documents relevant to this search reported that nanoemulsions loaded with essential oils and plant extracts from different botanical species had in vitro antimicrobial activity against different microorganisms of medical importance, in addition to enhancing the antimicrobial effects of these bioproducts. Therefore, nanostructured antimicrobials with essential oils and plant extracts can be considered treatment options for microbial diseases: due to their physicochemical properties, they act as better delivery vehicles for natural products with good bioavailability, by reducing toxicity and prolonging the useful life of these natural antimicrobials, thus enhancing treatment for infectious human diseases.
Background/Objectives: Nanoemulsions (NEs) possess properties that enhance the solubility, bioavailability and therapeutic efficacy of drugs. Chalcones are compounds known for their antifungal properties. In this study, we evaluated different emulsification techniques to create alginate nanoemulsions containing chalcone (1E,4E)-1,5-bis (4-methoxyphenyl) penta-1,4-dien-3-one (DB4OCH3). Our goal was to develop an antifungal formulation targeting Candida albicans strains. Methods: Ultrasound and ultrasound combined with high-speed homogenization techniques were used to prepare alginate-stabilized nanoemulsions. Particle size, zeta potential and encapsulation efficiency were evaluated. Additionally, in vitro release studies were conducted. Results: The combined emulsification technique produced stable nanoparticles with high encapsulation efficiency and antifungal activity, with a minimum inhibitory concentration of 8.75 μg/mL for the nanoemulsions compared to 312 µg/mL for free DB4OCH3. NEs’ effectiveness can be attributed to their ability to form nanodroplets efficiently, facilitating the solubilization of the chalcone in the oily phase. The particle size varied between 195.70 ± 2.69 and 243.40 ± 4.49 nm, with an increase in chalcone concentration leading to larger particle sizes. The zeta potential showed values from −91.77 ± 5.58 to −76.90 ± 4.44 mV. The UHS-7 sample exhibited an encapsulation efficiency of 92.10% ± 0.77, with a controlled in vitro release of 83% after 34 h. Molecular docking simulations showed that the aromatic nature of DB4OCH3 resulted in the formation of apolar interactions with aromatic residues located in the active site of the TMK, as observed in their respective co-crystallized inhibitors, within an affinity energy range that enables optimum specificity of the ligand for these two pathways. Pharmacokinetic analyses indicated high passive cell permeability and low hepatic clearance, and phase I metabolism reduces its oral bioavailability and metabolic stability, suggesting a promising active ingredient as an oral drug with control of the daily oral dose administered. Conclusions: The combined nanoemulsification technique led to the formation of finely dispersed nanodroplets that favored the solubilization of the chalcone in the oil phase, which led to a better performance in the antifungal properties. DB4OCH3 shows promise as an oral drug with controlled dosing.
The objective of this study was to synthesize and evaluate the in vitro activity of aminochalcones against Haemonchus contortus eggs and adults. Aminochalcones 1 and 2 were synthesized using Claisen–Schmidt condensation and characterized using Fourier-transform infrared spectroscopy, nuclear magnetic resonance, and mass spectrometry. The activity of both aminochalcones was assessed in the egg hatch test and that of aminochalcone 1 was further evaluated in the adult worm motility test using multiresistant H. contortus. The chemical structures of the synthesized compounds were confirmed, and changes induced in eggs and adults were assessed using scanning electron microscopy (SEM). Aminochalcones 1 and 2 inhibited larvae hatching by 98.70 and 99.89%, respectively, at concentrations of 0.25 and 1 mg/mL. SEM images revealed structural and morphological changes in eggs treated with both compounds. After 12 h of exposure to aminochalcone 1 (1.25 mg/mL), all adult nematodes were immobile, and wrinkling of the cuticle was observed. These findings indicate the ovicidal effect of aminochalcones and the inhibition of worm motility by aminochalcone 1. Our preliminary study demonstrated, for the first time, the anthelmintic activity of this class of compounds against gastrointestinal nematodes of small ruminants and suggest further anthelmintic evaluation.