Search Results (95)

(1) Background: Our study investigates the green synthesis of Ag₂O/Ag nanoparticles using the isoflavone Puerarin as a bioreductor. (2) Methods: The PUE@Ag₂O/Ag nanoparticles were characterized using various techniques, including X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FTIR), electronic microscopy (TEM, SEM), energy dispersive X-ray spectroscopy (EDX), and dynamic light scattering (DLS). Biological activities were assessed through antimicrobial testing, cytotoxicity assays on human keratinocytes and melanoma cells, and an in ovo screening using the HET-CAM assay. (3) Results: The formation of crystalline Ag₂O/Ag nanoparticles with sizes below 100 nm was accomplished with Puerarin. Despite their high cytotoxicity at all tested concentrations, the nanoparticles showed antioxidant activity with IC₅₀ 981.5 ± 94.2 μg/mL, antibacterial activity against several clinically relevant nosocomial strains (Streptococcus pyogenes, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa), and no local irritant effects or inhibition of angiogenesis in the HET-CAM assay. (4) Conclusions: This study provides insights into the synthesis, characterization, and biological profile of PUE@Ag₂O/Ag nanoparticles for potential biomedical applications. Full article

Skin disorders constitute a persistent health problem, covering both acute and chronic conditions that manifest in patients of all ages. Betulinic acid (BA) is a triterpene previously studied as an efficient treatment of skin ailments due to its innate pharmacological properties. Nonetheless, due to its lipophilic nature and low bioavailability, topical delivery systems are necessary for its proper administration. Oleogels are efficient carriers for the incorporation of hydrophobic biomolecules; however, their use for the delivery of BA remains scarce. Therefore, this study was designed to develop, characterize, and evaluate a BA-containing oleogel (BA-O) regarding its cutaneous safety profile as a potential pharmaceutical formulation targeting dermatologic issues. The findings illustrated the efficient formulation of BA as oleogel, the product presenting the specific conditions of topical semi-solid formulations in terms of physico-chemical characteristics and high biocompatibility in vitro and in ovo, as BA-O lacked a cytotoxic effect in HaCaT and JB6 Cl 41-5a skin cells (cell viability percentages being > 70%) and was categorized as non-irritant in EpiDerm™ tissues (viability > 80%) and on the chorioallantoic membrane (Irritation Score = 0.186). These results present the preclinical biosafety profile of BA-O with prospective potential for cutaneous applications that should be investigated in future studies. Full article

Hypericum perforatum L. (H.P.), a plant renowned for its wound-healing properties, was investigated for antioxidant/antimicrobial efficacy, toxicological safety, and in vivo wound-healing effects in this research to develop and characterize novel nanoemulsion hydrogel (NG) formulations. NG were prepared via emulsion diffusion–solvent evaporation and polymer hydration using Cremophor RH40 and Ultrez 21/30. A D-optimal design optimized oil/surfactant ratios, considering particle size, PDI, and drug loading. Antioxidant activity was tested via DPPH, ABTS⁺, and FRAP. Toxicological assessment followed HET-CAM (ICH-endorsed) and ICCVAM guidelines. The optimized NG-2 (NE-HPM-10 + U30 0.5%) demonstrated stable and pseudoplastic flow, with a particle size of 174.8 nm, PDI of 0.274, zeta potential of −23.3 mV, and 99.83% drug loading. Release followed the Korsmeyer–Peppas model. H.P. macerates/NEs showed potent antioxidant activity (DPPH IC₅₀: 28.4 µg/mL; FRAP: 1.8 mmol, Fe²⁺/g: 0.3703 ± 0.041 mM TE/g). Antimicrobial effects against methicillin-resistant S. aureus (MIC: 12.5 µg/mL) and E. coli (MIC: 25 µg/mL) were significant. Stability studies showed no degradation. HET-CAM tests confirmed biocompatibility. Histopathology revealed accelerated re-epithelialization/collagen synthesis, with upregulated TGF-β1. The NG-2 formulation demonstrated robust antioxidant, antimicrobial, and wound-healing efficacy. Enhanced antibacterial activity and biocompatibility highlight its therapeutic potential. Clinical/pathological evaluations validated tissue regeneration without adverse effects, positioning H.P.-based nanoemulsions as promising for advanced wound care. Full article

A comparative evaluation of Moringa oleifera Lam. ethanolic leaf extracts was performed using different extraction methods (maceration or ultrasound-assisted) and the qualitative and quantitative profile of the bioactive compounds contained were further assessed. The antioxidant potential and antimicrobial activity were evaluated, as well as the antiangiogenic effects through in ovo studies. Six ethanolic extracts were tested in this study. Moringa MAC 70% and Moringa US 70% extracts displayed the highest concentration of phenolic compounds and also showed a significant AOA at the highest tested dose. Regarding the antimicrobial effect, the extracts obtained with 70% ethanol (maceration or ultrasound-assisted) had antimicrobial activity against S. aureus, S. pyogenes and E. coli, followed by Candida parapsilosis. On the Pseudomonas aeruginosa strain, the extracts showed no effect. The HET-CAM assay showed that the extracts did not cause any irritation compared to the used positive control. Furthermore, the extracts Moringa MAC 70% and Moringa US 70% did not affect the normal process of blood vessel formation. The data obtained highlights that, from the six tested extracts, the ones obtained with 70% ethanol using maceration and ultrasound-assisted methods (Moringa MAC 70% and Moringa US 70%) showed the highest phenolic content and exhibited the strongest antioxidant activity. The same two extracts did not show signs of irritation in the HET-CAM model. Full article

Background: Cyclophosphamide (CP) chemotherapy is commonly associated with various side effects. The development of an effective therapy capable of counteracting these effects is of great interest. Objectives: We evaluated the effects of a novel polyherbal formulation (PHF) on CP cytotoxicity in TM3 cells and fictive ejaculation in rats, and determined its possible mechanism. Methods: The phytochemical analysis of PHF was determined by GC-MS. Various oxidative stress-related parameters (DPPH, ABTS⁺, CUPRAC, FRAP, MMP, and DCF-DA) and the cytotoxicity (hemolysis and HET-CAM) of PHF were evaluated. Its effect on fictive ejaculation was tested by recording the electromyographic activities of bulbospongiosus muscles, and the involvement of TRPV1/TRPM2 channels was investigated using their specific agonists and antagonists. Results: We found that PHF contained various phytocompounds. PHF prevented CP-induced oxidative stress in TM3 cells, probably due to its strong antioxidant potential. For instance, PHF inhibited apoptosis, lipid peroxidation, and ROS generation. Furthermore, the activities of capsaicin (CAP) and cumene hydroperoxide (CHPx) were significantly lowered by PHF, indicating TRPV1 and TRPM2 inhibition. In the in vivo study conducted in spinal male rats, the number of contractions of the bulbospongiosus muscles was significantly (p < 0.001) lowered in the PHF + DOPA (1.54 ± 0.3) and PHF + CAP (2.43 ± 0.74) groups, compared with the DOPA (8.75 ± 0.71) and CAP (7.41 ± 1.01) groups, respectively. Additionally, PHF delayed the pro-ejaculatory effects of dopamine (by 17.6%) and capsaicin (by 32.69%). The in silico study revealed a strong binding affinity between the selected PHF phytocompounds and the active pockets of TRPV1 and TRPM2. HET-CAM and hemolysis assays revealed no harmful effects of PHF. Conclusions: PHF prevented CP cytotoxicity in TM3 cells and delayed the pro-ejaculatory effects of dopamine and capsaicin in spinal rats through dopamine and TRPV1 inhibition. PHF could be a potential candidate for the management of CP chemotherapy-related disorders, such as premature ejaculation, in particular. Full article

Mild to moderate pain for a few hours to several days post-piercing is normal, and the pain is usually accompanied by swelling, redness, and warmth due to the inflammatory response. Cool compresses and over-the-counter analgesics (e.g., NSAIDs) can ease mild discomfort. However, oral NSAIDs may have systemic side effects; for this reason, we propose a topical anti-inflammatory approach. Four pranoprofen-loaded gels were created using different gelling agents: Sepigel^® 305 (PF-Gel-Sep), Carbopol^® 940 (PF-Gel-Car), Pluronic^® F-68 (PF-Gel-Plu), and Lutrol^® F-127 (PF-Gel-Lut). The gels were assessed for pH, morphology, FT-IR spectroscopy, rheological properties, spreadability, swelling and degradation, drug release kinetics, skin permeation (cow and human skin), irritation potential (HET-CAM assay), and impact on skin barrier function (TEWL and SCH). The gels exhibited varied rheological properties with PF-Gel-Car showing high viscosity and PF-Gel-Plu very low viscosity. All gels had similar spreadability with PF-Gel-Lut showing the highest. PF-Gel-Car showed the highest amounts of PF released, whereas PF-Gel-Plu led to the highest amount of pranoprofen retained in human and bovine skin. The HET-CAM assay indicated that none of the PF-Gels were irritating. Additionally, PF-Gel-Car and PF-Gel-Plu showed no cytotoxic effects on HaCaT cells. In vivo testing on mice showed that PF-Gel-Car prevented inflammation, while the rest of the gels were able to revert it in 25 min. Skin tolerance tests revealed the gels did not affect TEWL, and some gels improved SCH. The study successfully formulated and characterized four PF-loaded topical gels with potential to be used as an alternative for treating inflammation from piercings and ear tags. Full article

The bacterial contamination of eggshells may be responsible for embryonic mortality, as may the contamination of chicks and broilers. Poor incubation results may be related to high levels of contamination that overcome the antibacterial defenses of the eggshell structure and the poultry’s immune system. Although synthetic antibacterial formulations have demonstrated efficacy in controlling eggshell bacteria, they have also demonstrated toxicity to the embryo. In this study, we aimed to establish a safe and antibacterial topical protocol using Syzygium aromaticum essential oil (SAEO) to sanitize hatching chicken eggs. We evaluated the antibacterial capacity of this essential oil and used the ‘hen’s egg test on chorioallantoic membrane’ (HET-CAM) model to measure its toxicity. Our results demonstrated the high effectiveness of SAEO in reducing the bacterial load on eggshells, suggesting that this natural compound is a promising egg sanitizer. However, although the HET-CAM model did not indicate signs of toxicity for pure SAEO, we recommend that its application, following dilution in grain alcohol, be carried out on the surface of eggshells and never directly in the internal embryonic compartment, owing to the toxicity of alcohol. Full article

Background/Objectives: Conjugation techniques are increasingly valued in food chemistry for enhancing sensory properties, nutritional profiles, and bioactivity, with potential applications in cosmeceuticals. This study aimed to investigate the potential of Glycine max (L.) Merrill oligopeptide–monosaccharide conjugates as active ingredients in cosmeceuticals, emphasizing their biological activities and stability. Methods: G. max isolate was prepared and subsequently hydrolyzed using alcalase to obtain the oligopeptide (OP). The OP was then conjugated with allulose (AL) or mannose (MN) through a controlled humid-dry heating process to produce the conjugates, OPA and OPM, respectively. Their biological activities, including antioxidant, anti-tyrosinase, anti-collagenase, anti-elastase, and anti-hyaluronidase properties, were assessed and compared to the individual components. Additionally, the irritation potential was evaluated using the hen’s egg test on chorioallantoic membrane (HET-CAM). The stability was examined under varying pH levels, temperatures, and light conditions based on their biological activity profiles. Results: OPA demonstrated the highest antioxidant activity, showing the lowest DPPH^• IC₅₀ value of 198.6 ± 2.7 µg/mL along with a strong ferric reducing power of 1.37 ± 0.04 µg FeSO₄/g sample. Besides, OPM showed superior tyrosinase inhibition on both L-tyrosine and L-DOPA substrates, highlighting its potential for skin whitening. Both OPA and OPM significantly enhanced collagenase inhibition, supporting their anti-aging potential. All samples were non-irritating in the HET-CAM test. The conjugates (OPA and OPM) demonstrated enhanced stability against pH, heat, and light compared to OP, AL, and MN. Conclusions: Oligopeptide–monosaccharide conjugation not only improved bioactivity but also enhanced biological stability, suggesting their potential for use in cosmeceutical applications. Full article

(1) Background: Controlled skin perforations, such as ear tags, piercings, and microdermal implants, induce inflammation and stress in individuals undergoing these procedures. This localized trauma requires care to optimize healing, reduce inflammation, and prevent infections. (2) Methods: Two formulations were developed: an FB-suspension and an FB-gel. Their in vivo efficacy was evaluated, along with drug retention in porcine and human skin after 30 min of administration, chemical stability at different temperatures, cytotoxicity, histological changes induced via transdermal application, and irritative potential, assessed using the HET-CAM assay. (3) Results: Both formulations reduced inflammation when applied 30 min before perforation compared to the positive control. The FB-suspension demonstrated no cytotoxicity and exhibited greater efficacy than the free flurbiprofen solution, highlighting the advantages of using nanoparticle-mediated drug delivery. Moreover, the FB-gel maintained chemical stability for up to 3 months across a temperature range of 4 to 40 °C. Histologically, no significant changes in skin composition were observed. (4) Conclusions: The FB-suspension is viable for both pre- and post-perforation application, as it is a sterile formulation. In contrast, the FB-gel is a convenient and easy application, making it a practical alternative for use in both clinical and veterinary settings. Full article

Background/Objectives: Leishmaniasis is a neglected tropical disease caused by a protozoan parasite of Leishmania. This study aimed to evaluate the in vitro efficacy and toxicity of a previously developed amphotericin gel as a possible treatment for cutaneous leishmaniasis. Methods: First, quality control of the AmB-gel was carried out, including microbiological stability. The permeated and retained drug was tested on healthy and lacerated human skin. Tolerance to the AmB-gel was tested in vitro using HaCaT, RAW 264.7, and J774 cell lines and by an irritation test (HET-CAM). Promastigotes and amastigotes of various Leishmania species were tested, and the microscopic morphology of promastigotes exposed to the formulation was analyzed. Computational analysis was performed on the drug, polymer, and ergosterol in the promastigote. Results: The AmB-gel presented appropriate characteristics for topical use, including no microbial contamination after storage. The amount of drug retained on the intact and injured skin was 1180.00 ± 13.54 µg/g/cm² and 750.18 ± 5.43 µg/g/cm², respectively. The AmB-gel did not cause significant signs of toxicity. The IC₅₀ of the AmB-gel for promastigotes was less than 1 µg/mL for the four species examined, i.e., Leishmania infantum, Leishmania tropica, Leishmania major, and Leishmania braziliensis, and less than 2 µg/mL for amastigotes of Leishmania infantum and Leishmania tropica. The AmB-gel caused notable effects on the surface of promastigotes. Computational analysis revealed primarily hydrophobic and van der Waals interactions between AmB and Pluronic^® F127 and ergosterol. Conclusions: Based on the drug retention content and IC₅₀ values observed for both parasite stages, the AmB-gel may be a promising candidate for in vivo studies in patients with cutaneous leishmaniasis. Full article

Background: The low solubility and poor skin permeability of sulfasalazine (SLZ) present significant challenges for its effective topical delivery. The objective of the current investigation is to formulate a hydrogel-based SLZ-loaded cyclodextrin nanosponge for topical therapy in psoriasis. Methods: SLZ-loaded nanosponges were prepared by the melt polymerization method and evaluated for physiochemical characteristics, drug release, and cytocompatibility. The selected nanosponges (SLZ-NS4) were transformed to hydrogel and further evaluated for rheology, texture, safety, skin permeability, and in vivo for anti-psoriatic effect in mouse tail and imiquimod-induced psoriasis-like inflammation models in mice. Results: Physiochemical data confirms nanoscale architecture, drug inclusion in nanosponges, crystalline structure, and formulation stability. The release profile of SLZ-NS4 revealed sustained release behavior (22.98 ± 2.24% in 3 h). Cytotoxicity assays indicated negligible toxicity against THP1 cells, resulting in higher viability of cells than pure SLZ (p < 0.05). The HET-CAM assay confirmed the safety, while confocal laser scanning microscopy demonstrated deeper skin permeation of SLZ. In the mouse tail model, a remarkable decline in relative epidermal thickness, potential improvement in percent orthokeratosis, and drug activity with respect to control was observed in animals treated with SLZ-NS4 hydrogel. The efficiency of the developed SLZ-NS4-loaded hydrogel in treating psoriasis was confirmed by the decline in PASI score (81.68 ± 3.61 and 84.86 ± 5.74 with 1 and 2% w/v of SLZ-NS-HG). Histopathological analysis and assessment of oxidative stress markers revealed the profound anti-psoriatic potential of the fabricated SLZ-NS4 hydrogel. Conclusions: These findings highlight the profound potential of the developed delivery system as an effective topical therapy for psoriasis. Full article

The use of nanoparticles improves the stability, solubility, and skin permeability of natural compounds in skincare products. Based on these advantages, this study aimed to incorporate the Phlomis crinita extract into polymeric nanoparticles to improve its topical skin delivery for wound healing purposes. The study involved the preparation of nanoparticles of PLGA and PLGA-PEG (PCE-PLGA-NPs and PCE-PLGA-PEG-NPs) using the solvent displacement method, physicochemical and biopharmaceutical characterization, tolerance studies by the HET-CAM assay and evaluation of skin integrity parameters, and in vitro efficacy via a scratch wound healing experiment. The prepared nanoparticles were nanometer-sized with spherical form and demonstrated an encapsulation efficiency greater than 90%. The major component (luteolin) was released following a kinetic model of hyperbola for PCE-PLGA-PEG-NPs and one-phase exponential association for PCE-PLGA-NPs. Moreover, the important permeability of luteolin skin was observed, especially for PCE-PLGA-PEG-NPs. Both formulations exhibited no irritation and no damaging effects on skin integrity, suggesting their safety. Finally, the results of the scratch wound healing experiment using 3T3-L1 cells revealed significant cell migration and proliferation, with an improved efficacy for PCE-PLGA-PEG-NPs compared to the free extract, demonstrating the potential of this formulation in the treatment of wound healing. Full article

Nanoemulsions are significant for cosmetic products intended for skin care and for health products due to the reduced size (range 20 to 500 nm) of the globules, which avoids processes of instability. They present transparency, fluidity, wettability, and spreadability; increase skin penetration; and have good sensation. The main instability mechanism of nanoemulsions is called Ostwald ripening, responsible for increasing the average diameter of emulsion globules. Sesame Seed Oil (SO) and Raspberry Seed Oil (RO) are indicated as moisturizing agents recently used in the cosmetic industry and for reducing transepidermal water loss, preventing damage to the skin barrier. They contain specific compounds with common properties such as antioxidant, moisturizing, emollient, and photoprotective actions, making them attractive alternative and complementary treatments to soften the process of skin aging. Below, we present the results of this research on the development of nanoemulsions containing Sesame Seed Oil added with Raspberry Seed Oil by the low-energy method. SO nanoemulsions at HLB = 8.0 were obtained with PEG 15 castor oil (A) and PEG 30 castor oil (F.80) and had globule sizes of 50 nm and 200 nm, respectively, along with pH values considered suitable for skin care products and lower viscosity values allowing for the easy application of nanoemulsions to the skin. Nanoemulsions A and F.80 showed antioxidant activities of 68.71% and 67.75%, respectively. SO nanoemulsions with PEG 15 and PEG 30 castor oil were obtained at 85 °C and 75 °C, respectively, and have the lowest Ostwald ripening index (1.33 × 10²² m³ s⁻¹). The in vitro evaluation conducted using the HET-CAM method for nanoemulsions and PEG 15 and PEG 30 castor oils showed that they were slightly irritating and could be used in cosmetic products. Full article

The photosensitizer (PS) in the Photodynamic Therapy (PDT) field represents a key factor, being directly connected to the therapeutic efficacy of the process. Chlorin e6 is a second-generation photosensitizer, approved by the FDA with the most desired clinical properties for PDT applications, presenting high reactive oxygen species (ROS) generation and proven anticancer properties. However, hydrophobicity is a major limitation, leading to poor biodistribution. To overcome this condition, the present work developed an up-to-date nanoemulsion incorporating Ce6 in a new nanosystem (Ce6/NE). A comprehensive study of physicochemical properties, stability, fluorescence characteristics, the in vitro release profile, in vivo and ex vivo biocompatibility, and ex vivo efficacy was established. The nanoemulsions showed the desired particle size and stability over six months, with no spectroscopic or photophysical alterations. Uptake studies demonstrated the internalization of the Ce6/NE in monolayers, with biocompatibility at the lowest concentrations. The HET-CAM assay, however, revealed a higher biocompatibility range, also indicating Ce6/NE’s potential for cancer treatment through antiangiogenic studies. These findings highlight the use of a new promising photosensitizer for PDT modulated with nanotechnology that promotes low toxicity, higher bioavailability, and site-specific delivery. Full article

Amazonian fruit residues like piquia shells are often discarded despite their antioxidant potential for sustainable cosmetic use. This study evaluated the photostability, phototoxicity, and photoprotection of hydroalcoholic piquia shell extract (PqSE) combined with UV filters in solutions and cosmetic formulations. PqSE formulations were photostable, even stabilizing photounstable UV filters. Phototoxicity tests (OECD TG 432) showed no phototoxic potential (MPE < 0.15) and reduction in the phototoxic potential of UV filters, while ocular irritation potential via HET-CAM assay indicated no irritant effects. The extract combined with UV filters enhanced protection against UVA-induced reactive oxygen species (ROS) production, achieving 60.9% effectiveness, outperforming commercial photostabilizers. Against UVB radiation, it showed cellular viability above 80%, comparable to benzophenone-3. PqSE formulations exhibited a radical protection factor (RPF) nine times higher than controls and reduced radical production by 64% after visible/near-infrared (VIS/NIR) irradiation on porcine skin, compared to 38% for controls. Confocal Raman microspectroscopy showed penetration depths below 12 µm for all time points. This study highlights the potential of reusing fruit residues like PqSE as sustainable, effective ingredients in sunscreen formulations, offering enhanced photoprotection and reduced environmental waste. Full article