Polyphenols comprise a number of natural substances, such as flavonoids, that show interesting biological effects. Among these substances is naringin, a naturally occurring flavanone glycoside found in citrus fruits and Chinese medicinal herbs. Several studies have shown that naringin has numerous biological properties, including cardioprotective, cholesterol-lowering, anti-Alzheimer’s, nephroprotective, antiageing, antihyperglycemic, antiosteoporotic and gastroprotective, anti-inflammatory, antioxidant, antiapoptotic, anticancer and antiulcer effects. Despite its multiple benefits, the clinical application of naringin is severely restricted due to its susceptibility to oxidation, poor water solubility, and dissolution rate. In addition, naringin shows instability at acidic pH, is enzymatically metabolized by β-glycosidase in the stomach and is degraded in the bloodstream when administered intravenously. These limitations, however, have been overcome thanks to the development of naringin nanoformulations. This review summarizes recent research carried out on strategies designed to improve naringin’s bioactivity for potential therapeutic applications.

Leishmania braziliensis(L. braziliensis) causes cutaneous leishmaniasis (CL) in the New World. The costs and the side effects of current treatments render imperative the development of new therapies that are affordable and easy to administer. Topical treatment would be the ideal option for the treatment of CL. This underscores the urgent need for affordable and effective treatments, with natural compounds being explored as potential solutions. The alkaloid piperine (PIP), the polyphenol curcumin (CUR), and the flavonoid quercetin (QUE), known for their diverse biological properties, are promising candidates to address these parasitic diseases. Initially, the in vitro cytotoxicity activity of the compounds was evaluated using U-937 cells, followed by the assessment of the leishmanicidal activity of these compounds against amastigotes ofL. braziliensis. Subsequently, a golden hamster model with stationary-phaseL. braziliensispromastigote infections was employed. Once the ulcer appeared, hamsters were treated with QUE, PIP, or CUR formulations and compared to the control group treated with meglumine antimoniate administered intralesionally. We observed that the three organic compounds showed high in vitro leishmanicidal activity with effective concentrations of less than 50 mM, with PIP having the highest activity at a concentration of 8 mM. None of the compounds showed cytotoxic activity for U937 macrophages with values between 500 and 700 mM. In vivo, topical treatment with QUE daily for 15 days produced cured in 100% of hamsters while the effectiveness of CUR and PIP was 83% and 67%, respectively. No failures were observed with QUE. Collectively, our data suggest that topical formulations mainly for QUE but also for CUR and PIP could be a promising topical treatment for CL. Not only the ease of obtaining or synthesizing the organic compounds evaluated in this work but also their commercial availability eliminates one of the most important barriers or bottlenecks in drug development, thus facilitating the roadmap for the development of a topical drug for the management of CL caused byL. braziliensis.

In the context of addressing antimicrobial drug resistance in periocular infections, Tea Tree Oil (TTO) has emerged as a promising therapeutic option. This study aimed to assess the efficacy of TTO against bacterial strains isolated from ocular infections, with a particular focus on its ability to inhibit biofilm formation. Additionally, we designed and analyzed microcapsules containing TTO to overcome certain unfavorable physicochemical properties and enhance its inherent biological attributes. The quality of TTO was confirmed through rigorous analysis using GC-MS and UV-Vis techniques. Our agar diffusion assay demonstrated the effectiveness of Tea Tree Oil (TTO) against ocular bacterial strains, including Corynebacterium spp., coagulase-negative Staphylococcus spp., and Staphylococcus aureus, as well as a reference strain of Staphylococcus aureus (ATCC 25923). Notably, the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) for all tested microorganisms were found to be 0.2% and 0.4%, respectively, with the exception of Corynebacterium spp., which exhibited resistance to TTO. Furthermore, TTO exhibited a substantial reduction in biofilm biomass, ranging from 30% to 70%, as determined by the MTT method. Through the spray-drying technique, we successfully prepared two TTO-containing formulations with high encapsulation yields (80–85%), microencapsulation efficiency (90–95%), and embedding rates (approximately 40%). These formulations yielded microcapsules with diameters of 6–12 μm, as determined by laser scattering particle size distribution analysis, and exhibited regular, spherical morphologies under scanning electron microscopy. Importantly, UV-Vis analysis post-encapsulation confirmed the presence of TTO within the capsules, with preserved antioxidant and antimicrobial activities. In summary, our findings underscore the substantial therapeutic potential of TTO and its microcapsules for treating ocular infections.

Cannabidiol (CBD), extracted from Cannabis sativa L., holds therapeutic promise without inducing psychoactive effects seen with Δ9-tetrahydrocannabinol. Its interaction with the endocannabinoid system plays a pivotal role in regulating mood, pain perception and immune function. Nevertheless, CBD encounters hurdles in clinical application due to its poor bioavailability and water solubility. To overcome these limitations, researchers are exploring microencapsulation techniques, which involve encapsulating CBD within protective matrices. This comprehensive review offers insights into various microencapsulation methods for CBD, scrutinizing their advantages, limitations and implications for formulation optimization. By elucidating the potential of microencapsulation, this review underscores its promise in refining CBD therapy and addressing challenges associated with administration.

To evaluate the antibacterial and antibiofilm activities of sodium ibuprofenate (NaI) and its hypertonic variant (NaIHS) against multidrug-resistant Gram-negative bacteria (MDR-GNB) and explore their potential to inhibit β-lactamase enzymes. Antibacterial activity was assessed using minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), and time-kill assays. Antibiofilm activity was evaluated by measuring bacterial viability and biomass reduction in preformed biofilms. Scanning electron microscopy (SEM) was used to observe membrane effects. Molecular docking and molecular dynamics simulations were conducted to analyze the binding affinity of ibuprofen to the active sites of β-lactamases (CTX-M-15, KPC-2, OXA-23). NaI exhibited bactericidal activity at concentrations of 25-75 mm, with Acinetobacter baumannii being the most susceptible. NaCl (≥0.5 M) enhanced bactericidal efficacy and lowered MBCs. Time-kill assays indicated rapid bacterial eradication within 2 hours, with NaIHS achieving similar results at lower concentrations. SEM confirmed membrane disruption. Both formulations reduced bacterial viability in biofilms, with NaIHS showing greater efficiency. In silico studies suggest ibuprofen may inhibit β-lactamases, with enhanced interactions in saline environments. Sodium ibuprofenate, particularly in its hypertonic form, demonstrates strong antibacterial, antibiofilm, and potential β-lactamase inhibitory activity, making it a promising candidate for treating MDR-GNB infections.