Search Results (222)

Cutibacterium acnes is linked to the prevalent inflammatory skin disorder known as Acne Vulgaris (AV). Some topical agents exhibit unfavorable side effects like dryness and skin inflammation, and antimicrobial resistance (AMR) poses an increasing risk to effective AV management. This study develops and characterizes stable topical essential oil (EO)-loaded microemulgels with in vitro validated antimicrobial activities against C. acnes ATCC 6919, providing a solid scientific basis for their effectiveness. These microemulgels, with their potential to serve as an alternative to AMR-prone synthetic agents, could revolutionize the field of acne treatment. The MICs of the EOs (citronella, tea tree, and lemongrass) against C. acnes were determined. EO-loaded microemulgels were developed using a blend of microemulsion and carbopol/hyaluronic acid gel in a ratio of 1:1 and characterized, and their stability was observed over three months. The MICs of citronella, tea tree, and lemongrass EOs were 0.08, 0.16, and 0.62% v/v, respectively. The microemulgels were whitish and smooth, with characteristic EO odors. They demonstrated pH values ranging between 4.81 ± 0.20 and 5.00 ± 0.03, good homogeneity, a spreadability of 9.79 ± 0.6 and 12.76 ± 0.8 cm², a viscosity of 29,500 and 31,130 cP, and retained stability at 4, 25, and 40 °C. EO-loaded microemulgels were developed with the potential of C. acnes management. The formulation shows adequate potential for further pharmaceutical development towards translational adoption in acne management. Full article

Embedded printing of soft materials relies on yield-stress support matrices to prevent sagging and enable freeform fabrication. The rheological parameters of the matrix material directly influence critical printing outcomes such as strand positioning, cavity formation, structural stability, and defect suppression in embedded printing. Despite widespread use of Carbopol^® formulations, a systematic rheological characterization of ETD2020 across relevant polymer concentrations and pH levels for embedded printing is lacking. Here, we implement a full-factorial design with polymer concentrations from $0.1\mathrm{wt}\%$ to $0.9\mathrm{wt}\%$ and triethanolamine dosages of 30–$50$µL per $100\mathrm{g}$. Steady-shear ($0.001$–$200{\mathrm{s}}^{-1}$) and oscillatory ($1\mathrm{Hz}$) rheometry yielded Herschel–Bulkley parameters ${\tau }_y$, k, n as well as storage and loss modulus $G^{\prime }$/$G^{\prime \prime }$. All formulations exhibited pronounced shear-thinning, with ${\tau }_y$ increasing nonlinearly from <$1\mathrm{Pa}$ to $41.1\mathrm{Pa}$ and $G^{\prime }$ reaching $\approx 400\mathrm{Pa}$ at $0.9\mathrm{wt}\%$. A five-hour window of invariant rheology was identified, followed by a $\Delta {\tau }_y\approx 10\mathrm{Pa}$ increase after five days, indicating delayed polymerization. The comprehensive material characterization defines a rheological window for ETD2020 and facilitates simulation-based modeling and the targeted tuning of matrix properties. Heatmaps provide an interpolated depiction of combined carbomer and triethanolamine concentrations, enabling tunable support matrices for embedded printing. Full article

This study investigates the influence of different light sources (sunlight, green, red, and white LED) on the germination of Raphanus sativus L. sprouts and the potential use of their sprout extracts in the development of natural dermatocosmetic gels. The bioactive fractions were extracted using simple methods and analyzed for total polyphenol content and antioxidant activity. Statistical analysis of weight, total phenolic content, and antioxidant activity of Raphanus sativus L. sprouts was performed using ANOVA. Sprouts exposed to green LED light showed the highest biomass (16.13 ± 0.38 g), while red LED light resulted in the highest total polyphenol content (3.28 ± 0.03 mg GAE/g fresh weight). The highest antioxidant activity (6.60 ± 0.08 mM Trolox/g fresh weight) was obtained under white LED. Although variations were observed, ANOVA analysis revealed that only sprout weight differed significantly among treatments (p < 0.001), while differences in polyphenol content and antioxidant activity were not statistically significant (p > 0.05). The extract with the highest antioxidant activity was incorporated as an active ingredient into Carbopol-based hydrogel formulations containing natural gelling agents and gentle preservatives. The resulting gels demonstrated favorable pH (4.85–5.05), texture, and stability. The results indicate that the light spectrum influences the germination process and the initial development of seedlings. Moreover, radish sprout extracts, rich in bioactive compounds, show promise for dermatocosmetic applications due to their antioxidant, soothing, and antimicrobial properties. This study supports the use of natural resources in the development of care products, in line with current trends in green cosmetics. Full article

Background/Objectives: Coronaviruses (CoVs) are a large family of respiratory viruses that cause respiratory illnesses ranging from mild colds to severe diseases such as severe acute respiratory syndrome and pandemics. The nasal cavity is a primary site for CoV entry and transmission. The study aimed to prepare a novel mucoadhesive emulgel specifically formulated with simple, safe, and cost-effective excipients to create a barrier on the nasal mucosa that impedes CoV infection. This formulation strategy was specifically designed to enable rapid and straightforward in vivo translation, addressing a critical gap in preventive measures against respiratory viruses. Methods: Three emulgels, containing macadamia oil, Carbopol and different percentages of hydroxypropyl methylcellulose (1, 1.2 and 1.5% (w/v), HPMC), were properly prepared and characterized for mucoadhesion, viscosity, and spreadability. The biological activity against SARS-CoV-2 was evaluated in vitro on infected epithelial cells. Results: The emulgel with 1.2% HPMC demonstrated optimal physicochemical properties (mucoadhesion: 342 ± 9 mN/cm²; viscosity: 1080 ± 83 cp; spreadability: 7.27 ± 0.06 cm) suitable for nasal application. Importantly, in vitro biological assays demonstrated that this emulgel significantly inhibits SARS-CoV-2 infection in epithelial cells, indicating an effective barrier to viral diffusion. Conclusions: By employing readily available, safe, and inexpensive excipients, this novel mucoadhesive emulgel offers a practical, scalable, and rapidly translatable nasal prophylactic approach to prevent early SARS-CoV-2 infection, addressing a critical unmet need in pandemic preparedness. Full article

Background: Anthralin is known for its efficacy in treating psoriasis and acne, possessing poor solubility. Addressing these limitations, the present study endeavors to develop a microemulgel formulation of anthralin aimed at enhancing solubility. Method: The solubility study was performed in various solvents. An o/w (oil-in-water) emulsion was formed using the water titration method, which was optimized by statistical experimental design half-run CCD. The final optimized batch was evaluated for physicochemical and in vitro properties Result: The final optimized batch showed a particle size (PS) of 417 nm, −25.2 mV zeta potential (ZP) and pH 5.8, which remained stable upon centrifugation, heating–cooling and freeze–thawing cycle. Furthermore, microemulsion with Carbopol 943 5% w/v was selected as the gel base for the formation of microemulgel characterized by PS, ZP, pH, and viscosity of 230 nm, −50.6 mV, 6.9 and 14,200 cps, respectively, that ensured it a high enough stability. In silico molecular docking between ligand and protein provides the binding energies validating the interaction. Hence, the in silico study was performed for psoriasis and P. acne proteins. An in vitro antibacterial activity study on Propionibacterium revealed a significant efficiency of the formulation and MTT assay using L929 cell line in the presence of the drug-loaded microemulgel indicated an inhibition of growth proving that formulation has anti-psoriatic activity. Conclusions: Combination therapy with Clindamycin might improve efficacy while reducing antibiotic resistance risks. Full article

Background:Cenostigma bracteosum (Tul.) Gagnon & G.P. Lewis (Fabaceae), popularly known as “catingueira”, is a plant widely distributed in the Caatinga biome, which comprises 11% of the Brazilian territory. While this species is of interest given local knowledge, formal reports are lacking in the literature, warranting targeted investigation. This study aimed to prepare and characterize a hydroethanolic extract of C. bracteosum leaves, prepare carbopol gels containing the extract, and evaluate their cytotoxicity and antibacterial activity against Staphylococcus aureus and Escherichia coli. Methods: The initial extract was prepared in an ultrasonic bath using ethanol/water (70:30, v/v). The extract (1 mg/mL) was analyzed by liquid chromatography coupled with mass spectrometry (UHPLC-MS/MS). Carbopol-based gels containing 1% and 3% of C. bracteosum extract were prepared and characterized in terms of pH, conductivity, spreadability, and rheology. The cytotoxicity was determined by the MTT method using MC3T3-E1 pre-osteoblast cells and L929-CCL1 fibroblast cells. The antibacterial activity of the extract and gels was evaluated using the agar diffusion method against S. aureus and E. coli. Results: The C. bracteosum leaves extract demonstrated antibacterial activity against S. aureus and E. coli, were not cytotoxic for the assessed cells at concentrations up to 100 μg/mL, and its analysis by UHPLC-MS/MS allowed the annotation of 18 metabolites, mainly of the phenolic acid and flavonoids glycoside classes, together with a biflavonoid. The prepared gels remained stable over the 30-day post-production analysis period. Conclusions: These findings provide a better understanding of the chemical diversity of the secondary metabolites of a common Caatinga biome species—C. bracteosum—specifically present in leaves hydroethanolic extract and gel formulation adapted for skin application with activity against S. aureus. Full article

Background/Objectives: Raynaud’s phenomenon (RP) is characterized by an exaggerated vasoconstrictive response of small blood vessels in the fingers and toes to cold or stress. Oral therapy with tadalafil (TDL), a phosphodiesterase-5 inhibitor, is limited by systemic side effects and reduced patient compliance. This study aimed to develop and evaluate a TDL-loaded nanoemulgel for transdermal delivery as a non-invasive treatment alternative for cold-induced vasoconstriction. Methods: TDL-loaded nanoemulsions were prepared using the aqueous titration method with cinnamon oil as the oil phase and Cremophor RH40 and Transcutol as the surfactant–cosurfactant system. The optimized nanoemulsion was incorporated into a carbopol-based gel to form a nanoemulgel. The formulation was characterized for droplet size, morphology, thermodynamic stability, rheological properties, in vitro drug release, skin permeation, and pharmacokinetic behavior. Infrared thermography was employed to assess in vivo efficacy in cold-induced vasoconstriction models. Results: The optimized TDL nanoemulsion exhibited a spherical morphology, a nanoscale droplet size, and an enhanced transdermal flux. The resulting nanoemulgel displayed suitable physicochemical and rheological properties for topical application, a short lag time (0.7 h), and a high permeability coefficient (Kp = 3.59 × 10⁻² cm/h). Thermal imaging showed significant vasodilation comparable to standard 0.2% nitroglycerin ointment. Pharmacokinetic studies indicated improved transdermal absorption with a higher C_max (2.13 µg/mL), a prolonged half-life (t_1/2 = 16.12 h), and an increased AUC_0–24 compared to an oral nanosuspension (p < 0.001). Conclusions: The developed TDL nanoemulgel demonstrated effective transdermal delivery and significant potential as a patient-friendly therapeutic approach for Raynaud’s phenomenon, offering an alternative to conventional oral therapy. 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

Caffeine is a well-known xanthine that possesses antioxidant effects that could contribute to its application in different skin disorders. In order to enhance its effects, approaches for improving its permeation and penetration through skin layers could be applied. This study emphasizes the preparation of caffeine–cyclodextrin complex and its formulation in carbopol hydrogel. The complex was developed at a 1:1 molar ratio between caffeine and hydroxypropyl-β-cyclodextrin. It was found that the complex enhanced the radical scavenging activity of caffeine against ABTS radical as well as the protective effects against H₂O₂-induced oxidative stress in L929 fibroblasts. Then, the complex was formulated in hydrogel by applying 1% carbopol. The spreadability and penetration of the loaded hydrogel were improved in comparison with the empty hydrogel. The results revealed that the system could be appropriate for therapies of skin disorders, and its wound healing abilities could be further investigated. Full article

Background: Trichophyton indotineae terbinafine-resistant infections are emerging in healthy individuals. Luliconazole, an imidazole antifungal that is effective against skin infections, faces challenges due to low water solubility and poor skin penetration. This study aimed to formulate a luliconazole-loaded nanostructured lipid-carrier (NLC) gel in a Carbopol-based system to enhance drug absorption and efficacy in a guinea pig model of dermatophytosis. Methods: Luliconazole-loaded nanostructured lipid carriers (NLCs) were prepared using a solvent evaporation method and gel formulation. Skin absorption and retention were assessed via Franz diffusion cells. The antifungal efficacy was tested against T. indotineae in thirty guinea pigs with induced tinea corporis, divided into five treatment groups. Mycological, clinical, and histopathological evaluations were conducted, along with skin irritation studies for safety. Results: LCZ-NLC demonstrated significantly better skin penetration than simple luliconazole gel, with cumulative drug penetration of 71.8 ± 3.7 μg/cm² versus 50.9 ± 4.2 μg/cm² after 24 h. Both formulations achieved complete infection resolution after 21 and 28 days, with reduced inflammation and no local irritations. On day 21, the LCZ-NLC 1% gel significantly reduced lesion scores and mycological evidence of infection compared to the terbinafine-treated groups, untreated controls, and NLC-gel-treated group (p < 0.05). Histopathological analysis indicated a reduction in both epidermal thickening and fungal burden in the models that received treatment with the LCZ-NLC 1% gel. Conclusions: Luliconazole-loaded lipid carriers enhance drug absorption and efficacy, suggesting shorter treatment durations and improved patient outcomes for resistant fungal infections. However, further studies are warranted to correlate these findings with clinical outcomes. Full article

Malignant skin conditions are classified as the most common forms of cancer, with an evolution of one million new cases reported every year. Research efforts in the medical field are focused on developing innovative strategies for the dissemination of measures for preventing cancer and providing new antitumor compounds. The present research examines the development and evaluation of 1% Carbopol-based hydrogels incorporating two porphyrin derivatives—5,10,15,20-tetrakis-(4-acetoxy-3-methoxyphenyl) porphyrin (P2.1) and 5-(4-hydroxy-3-methoxyphenyl)-10,15,20-tris-(4-acetoxy-3-methoxyphenyl) porphyrin (P2.2)—to create formulations suitable for topical photodynamic therapy (PDT) applications. The physicochemical properties of the obtained hydrogels were carefully evaluated, revealing the successful integration of the porphyrins into the 1% Carbopol hydrogel matrix. Rheological analysis demonstrated pseudoplastic behavior, with an increase in viscosity properties for P2.1 and P2.2, suggesting interactions with the Carbopol polymer structure. UV-visible and fluorescence spectroscopy confirmed the maintenance of the porphyrins’ photodynamic properties, essential for therapeutic efficacy. Pharmacotechnical studies highlighted the hydrogels’ suitability for topical applications. The formulations maintained an optimal pH range, ensuring skin compatibility and minimizing the potential for skin irritation. Their mechanical properties, including elasticity and rigidity, provided stability during handling and application. The high swelling capacity indicated effective moisture retention, enhancing skin hydration and drug release potential. Furthermore, the hydrogels demonstrated excellent spreadability, enabling uniform application and coverage, crucial for efficient light activation of the photosensitizers. The combination of robust physicochemical and pharmacotechnical properties highlights the potential of these porphyrin-loaded 1% Carbopol hydrogels as promising carriers for topical PDT. These results permit further biological and therapeutic investigations to optimize the formulation for clinical use, advancing the development of effective localized photodynamic therapies. Full article

Background: Rheumatoid arthritis is a chronic autoimmune disease that leads to severe disability and requires improved therapeutic strategies to optimize anti-inflammatory treatment. This study aimed to address this challenge by developing and characterizing an extended-release polymer matrix tablet containing ketoprofen and a ketoprofen–β-cyclodextrin complex with enhanced therapeutic properties. The objective was to improve inflammation management and therapeutic outcomes using a novel delivery system based on the inclusion of the active substance in cyclodextrin complexes. Methods: Tablets were formulated using ketoprofen and ketoprofen–β-cyclodextrin complexes combined with hydrophilic polymers such as Carbopol^® 971P NF, Kollidon^® VA 64, and Methocel^TM K4M. The complexes were obtained via the coprecipitation method to improve bioavailability. The kinetics of the release of ketoprofen, ketoprofen–β-cyclodextrin complex (2:1), and ketoprofen–β-cyclodextrin complex (1:1) from the tablets were investigated in vitro in artificial gastric and intestinal fluids, and drug release profiles were established. Advanced mathematical models were used to describe the nonlinear behavior of the drug–polymer systems. Results: The inclusion of ketoprofen in the β-cyclodextrin complexes was confirmed, revealing distinct release profiles. Tablets (K-3 F-3) containing the 1:1 complex showed rapid release (96.2% in 4–7 h), while tablets (K-1 F-4) containing free ketoprofen released 76% over 9–11 h. Higher polymer concentrations slowed the release due to gel barrier formation. Pharmacotechnical and stability tests supported their suitability as extended-release forms. A multifractal modeling approach described the release dynamics, treating the polymer–drug matrix as a complex system, with release curves characterized by variations in the fractal dimension and resolution. Conclusions: Specific hydrophilic polymer combinations effectively prolonged ketoprofen release. The developed matrix tablets, which were evaluated via in vitro studies and mathematical modeling, show promise for improving therapeutic outcomes and patient compliance during rheumatoid arthritis treatment. Full article

Levisticum officinale (lovage) is an aromatic and medicinal plant traditionally used for its antioxidant, anti-inflammatory and antimicrobial properties. The aim of this study was to evaluate the phytochemical composition and antioxidant activity of hydroalcoholic extracts obtained from leaves, roots and the whole plant, as well as to develop hydrogels with pharmaceutical potential. The hydroalcoholic extracts (70% ethanol) were characterized by spectrophotometric and HPLC-DAD methods to determine the total content of phenolic compounds, phenolic acids, flavonoids and condensed tannins. The antioxidant activity was evaluated by DPPH and ABTS methods. The extracts were included in 2% carbopol-based hydrogels and tested for stability and antioxidant efficacy. The hydroalcoholic extract of the leaves showed the highest content of total phenolic compounds (20.84 ± 2.18 mg GAE/g), total flavones (11.39 ± 2.48 mg QE/g) and condensed tannins (1.98 ± 1.55 mg CE/g), and was also the richest in quercetin (3.32 ± 1.25 mg/g), kaempferol (1.84 ± 1.63 mg/g), luteolin (2.12 ± 1.19 mg/g), rutin (4.38 ± 1.84 mg/g) and apigenin (1.91 ± 1.44 mg/g). The root extract had the highest content of phenolic acids, including ferulic acid (3.86 ± 1.37 mg/g), vanillic acid (2.53 ± 1.76 mg/g) and caffeic acid (3.28 ± 1.28 mg/g). The antioxidant activity was highest in the leaves extract, with values of 276.2 ± 3.4 µmol TE/g (ABTS) and 246.4 ± 3.6 µmol TE/g (DPPH). The whole-plant extracts showed intermediate values, offering a balance between flavonoids and phenolic acids. Hydrogels formulated with 5% extracts demonstrated stability and sustained antioxidant activity over time. Leaf extracts, due to their high flavonoid content, are recommended for formulations with antioxidant and photoprotective effects, while root extracts are suitable for anti-inflammatory and antimicrobial applications. Hydrogels obtained based on 2% carbopol represent a promising delivery system for dermato-cosmetic and pharmaceutical applications because they exhibited significant antioxidant action. Full article

Background: We previously reported that carbopol hydrogels incorporating indomethacin nanoparticles (IMC NPs) improved the low permeability and bioavailability of skin formulations in transdermal drug delivery systems. However, the combination of NPs with other types of hydrogels has not been sufficiently explored to date. Therefore, this study investigated propylene glycol (PG)/polyvinyl alcohol (PVA) hydrogel as an alternative base to carbopol hydrogel for incorporating IMC NPs. Methods: IMC NPs were prepared using bead milling treatment, and these NPs were incorporated into PG/PVA hydrogel (IMC-NP@PG/PVA hydrogel). The IMC concentration was measured using the HPLC method, and seven-week-old Wistar rats were used to evaluate skin absorption. Results: Bead milling reduced the IMC particle size in the PG/PVA hydrogels to the nanoscale (30–200 nm) without altering its crystalline form. The IMC-NP@PG/PVA hydrogel exhibited enhanced uniformity, solubility, and drug release compared to the IMC microparticle-loaded PG/PVA hydrogel (IMC-MP@PG/PVA hydrogel), with a 1.44-fold greater area under the concentration–time curve. Transdermal permeability studies revealed that IMC-NP@PG/PVA had 2.36-fold higher absorption than the IMC-MP@PG/PVA hydrogel, with dissolved IMC permeating the skin. Pharmacokinetics in the rats showed significantly increased plasma levels, absorption rates, and bioavailability for IMC-NP@PG/PVA, demonstrating its superior delivery efficiency. Moreover, the skin absorption of IMC-NP@PG/PVA was higher than that of carbopol hydrogel. Conclusions: These findings highlight the potential of PG/PVA hydrogels as an effective base for transdermal drug delivery systems based on NPs. Full article

Niosomes are a stable vesicular system composed of non-ionic surfactants and cholesterol, offering advantages such as enhanced stability and controlled drug release. In this study, a niosomal nanogel loaded with Ebastine was developed to improve patient compliance in treating skin allergic reactions. Thin-film hydration was employed to prepare niosomes using cholesterol, Span 60, Tween 80, and Ebastine, optimized via Box–Behnken experimental design. A dispersion method incorporating Carbopol 934 was utilized to create a niosomal gel, ensuring effective therapeutic outcomes. The formulation exhibited high drug entrapment efficiency (84.19%), a zeta potential of −27 mV, and vesicle sizes ranging from 100 to 300 nm. Evaluation included FTIR for drug–excipient compatibility, pH assessment, in vitro drug release studies, and stability testing, all yielding acceptable results. The encapsulation of Ebastine within niosomes is driven by critical physicochemical interactions between the drug, cholesterol, and surfactants. These interactions influence the stability, encapsulation efficiency, and release profile of the drug from the niosomal bilayer. Microbial studies indicated significant antimicrobial activity against S. aureus, underscoring its potential as an effective transdermal treatment for skin allergies. Full article