Search Results (147)

The aim of this study was to prepare curcumin/2-hydroxypropyl-β-cyclodextrin (HPβCD) inclusion complex, evaluate the antioxidant and antimicrobial activities of curcumin and curcumin in inclusion complex, as well as to examine the effect of curcumin and curcumin inclusion complex on the textural properties of Carbopol^® gel mixture. Curcumin/2-hydroxypropyl-β-cyclodextrin inclusion complex was prepared using the co-precipitation method in a molar ratio of 1:1. The antioxidant activity of curcumin and curcumin in inclusion complex was determined using DPPH, ABTS, and FRAP methods. The micro-dilution method was used to examine in vitro the antimicrobial activity of curcumin and curcumin in inclusion complex. The textural, rheological, and morphological properties of the samples (Gel 1- Carbopol^® gel; Gel 2- Carbopol^® gel with dispersed curcumin inclusion complex; Gel 3- Carbopol^® gel with dispersed curcumin) were examined. The textural properties were evaluated using a texturometer CT3 Texture Analyzer by means of a Texture Profile Analysis (TPA) test. The results showed that curcumin in inclusion complex had higher antioxidant and antimicrobial activity. The SEM confirms the presence of curcumin and inclusion complex in Carbopol^® gel. The rheological analysis confirmed that the structural integrity of Carbopol^® gel was preserved. The highest swelling degree is achieved by Gel 3 formulation. The in vitro release of curcumin from Gel 2 and Gel 3 occurs at the rates of 0.414 µg/h·g_gel and 0.376 µg/h·g_gel, respectively. The textural analysis showed that adding curcumin or its inclusion complex did not significantly change the properties of Carbopol^® gel, indicating potential for topical use. Full article

Background: Isoconazole nitrate (ISN), an antifungal agent that inhibits ergosterol synthesis by blocking lanosterol 14α-demethylation, is widely used to treat candidiasis, and improving its skin retention and permeability can enhance its therapeutic efficacy. Therefore, we developed an ISN nanoparticle (ISN-NP) gel by wet-bead milling in the presence of methylcellulose (MC). Methods: These ISN nanoparticles were incorporated into a carboxypolymethylene hydrogel (Carbopol). The ISN concentration was measured using HPLC, and Wistar rats and Candida albicans were used to evaluate skin absorption and antifungal activity, respectively. Results: The ISN-NP gel exhibited a particle size distribution ranging from 60 to 220 nm, with the nanoparticles remaining stable. In addition, the ISN-NP gel demonstrated superior antifungal activity against Candida albicans. The Carbopol gel maintained appropriate viscosity and physical stability, and the ISN nanoparticles were released from the gel. Compared with microparticle-based gels (ISN-MP gels), the ISN-NP gel showed significantly enhanced drug release and transdermal permeation, with 1.54- and 1.7-fold increases, respectively. Conclusions: These findings indicate that incorporating ISN nanoparticles (nanocrystalline ISN) into a Carbopol-based gel matrix provides a promising strategy to enhance the topical delivery of this poorly water-soluble antifungal drug. Overall, this nanogel system represents a valuable platform for transdermal delivery in clinical applications. Full article

Sertaconazole nitrate (SN), a broad-spectrum antifungal agent, is clinically employed against diverse dermatophyte infections. Its therapeutic efficacy, however, is constrained by poor aqueous solubility (0.006 mg/mL) and insufficient skin penetration from current commercial formulations. To address these limitations, this research focused on developing, optimizing (using a 3² factorial design), and assessing a topical nanovesicular gel incorporating sertaconazole nitrate-loaded ultraflexible liposomes (SN-UFLs) to enhance antifungal performance. The vesicles exhibited near-spherical morphology, with sizes ranging from 104.40 ± 1.20 to 151.90 ± 2.14 nm, zeta potential (ZP) values between −21.50 ± 1.25 and −51.20 ± 2.25 mV, and entrapment efficiency (EE) values from 77.60 ± 2.50% to 86.04 ± 3.20%. The optimized SN-UFL formulation (OPT-SN-UFL) was then integrated into a carbopol gel base. This SN-UFL-Gel was characterized for pH (6.5 ± 0.20), viscosity (499.66 ± 15 cP), spreadability (205 ± 1.50%), extrudability (154.18 ± 2.48 g/cm²), and drug content (96.7 ± 2.50%), as well as ex vivo skin permeation, skin irritation potential, and in vitro and in vivo antifungal efficacy. Compared with the marketed formulation, higher drug permeation and skin deposition were observed for SN-UFL-Gel. The SN-UFL-Gel exhibited a larger zone of inhibition (25 ± 1.50 mm) against Candida albicans compared to the commercially available formulation (20 ± 1.72 mm). The in vivo animal studies showed that SN-UFL-Gel showed better antifungal activity by efficient inhibition of infection induced in rats with Trichophyton mentagrophytes. The SN-UFL-Gel showed no signs of skin irritation and was stable at 4 ± 1, 25 ± 2, and 40 ± 2 °C for 3 months. Conclusively, the current work divulged successful augmentation of the overall effectiveness of sertaconazole nitrate by using deformable liposomes as a promising nanocarrier. Full article

The utility of bioresponsive multifunctional hydrogel compositions for biomedical applications is rapidly increasing due to the diverse array of biological stimuli that can profoundly alter physicochemical gel properties that benefit therapeutic interventions. The purpose of this research is to explore a bioresponsive hydrogel as a drug-free bioengineering concept to fortify the natural physical contraceptive barriers at the cervicovaginal junction. The results of this research demonstrate that a hydrogel comprising 4% (w/w) Carbopol^® 974P and 4% (w/w) polyvinylpyrrolidone (CP4%/PVP4%) undergoes bioresponsive structural changes in the presence of simulated seminal fluid, pH 7.7, (SFS) that increases the work required to spread the gel under physiologically relevant vaginal conditions. Combination of this bioresponsive hydrogel with liquified human semen at a volumetric ratio of 1:5 dramatically reduces in vitro sperm migration by 97%. Simultaneously, total sperm motility decreases from 72.0 ± 9.9% to 7.9 ± 13.7%, which is significantly below the WHO criteria defined for male fertility. Safety assessments performed in vitro and in vivo underline a robust vaginal safety profile comparable to approved vaginal products. Moreover, the results from an exploratory animal study performed with female New Zealand White rabbits suggest that the drug-free physical barrier established intravaginally after exposure of the bioresponsive CP4%/PVP4% hydrogel to alkaline semen seems at least equivalent in the prevention of pregnancy in vivo to the VCF^® Gel (Apothecus Pharmaceuticals, Ronkonkoma, NY, USA), a marketed spermicidal on-demand product containing nonoxynol-9. Full article

Background: Skin infections caused by Staphylococcus aureus represent a major public health concern, and plant extracts, such as those from Cochlospermum regium, have emerged as promising therapeutic alternatives. Methods: This study developed carbopol-based gel formulations containing ethanolic leaf extracts of C. regium (CRG 0.5% and 1%) and evaluated their physicochemical stability, antibacterial activity against S. aureus and a methicillin-resistant wound isolate, antioxidant potential, and biocompatibility. Results: Both CRG 0.5% and 1% were physically stable and maintained antibacterial activity for up to 90 days at 8 °C, while at 25 °C only CRG 1% retained activity throughout the evaluation period. In ex vivo pig skin assays, CRG 1% reduced methicillin-resistant S. aureus contamination by 99%, outperforming the conventional topical antibacterial agent (neomycin + bacitracin), which achieved 66% inhibition. The extract also exhibited high antioxidant activity without mutagenic or hemolytic effects. Although phenolic and flavonoid contents decreased over time, CRG 1% preserved adequate levels for therapeutic application. Conclusions: These findings indicate that CRG 1% has potential as a stable, safe, and effective alternative for the treatment of topical infections, particularly those caused by methicillin-resistant S. aureus. Full article

This study explores an innovative delivery strategy for the management of skin conditions: lipid nanosystems incorporated into a gel matrix. Echinacea purpurea extract, known for its antibacterial, antioxidant, and wound-healing properties, was encapsulated into lipid-based nanosystems and subsequently incorporated into Carbopol-based gel. The extract, rich in chicoric and caftaric acids, exhibited strong antioxidant activity (IC₅₀ = 56.9 µg/mL). The resulting nanosystems showed nanometric size (about 200 nm), high entrapment efficiency (63.10–75.15%), and excellent short-term stability. Superior biocompatibility of the nanosystems, compared to the free extract, was demonstrated using an MTS assay on L-929 fibroblasts. Moreover, the cytoprotective potential of the lipid carriers was evident, as pre-treatment significantly increased cell viability under H₂O₂-induced oxidative stress. These findings suggest that lipid-based encapsulation enhances the therapeutic profile of E. purpurea. The optimal lipid formulation was incorporated into a Carbopol-based gel, which demonstrated an appropriate pH (5.15 ± 0.75), favorable textural properties, sustained polyphenol release, and overall good stability. This research highlights the potential of plant-derived bioactives in the development of dermatocosmetic products, aligning with current trends in eco-conscious and sustainable skincare. Full article

Background/Objectives: Encouraged by the traditional use of Cotinus coggygria Scop. (European smoketree) for its anti-inflammatory and antioxidant properties, and considering the limitations of current therapies for recurrent aphthous stomatitis (RAS), we aimed to develop and evaluate a mucoadhesive oral gel containing C. coggygria stem bark extract. Methods: A thermosensitive gel was formulated using Carbopol^® 974P NF and poloxamer 407, enriched with 5% C. coggygria extract (CC gel), and characterized for its organoleptic properties, pH, electrical conductivity, and storage stability over six months. Therapeutic efficacy was assessed in a Wistar albino rat model of chemically induced oral ulcers. Animals were divided into three groups: untreated controls (CTRL), rats treated with gel base (GB), and those treated with CC gel over a 10-day period. Healing progression was monitored macroscopically (ulcer size reduction), biochemically (oxidative stress markers in plasma and tissue), and histologically. Results: The CC gel demonstrated satisfactory physicochemical stability and mucosal compatibility. Moreover, it significantly accelerated ulcer contraction and achieved complete re-epithelialization by day 6. Biochemical analyses revealed reduced TBARS and increased SOD, CAT, and GSH levels in ulcer tissue, indicating enhanced local antioxidant defense. Histological evaluation confirmed early resolution of inflammation, pronounced fibroblast activity, capillary proliferation, and full epithelial regeneration in the CC group, in contrast to delayed healing and persistent inflammatory infiltration in the GB and CTRL groups. Conclusions: These findings indicate that the CC gel has potential as a natural, topical formulation with antioxidant and regenerative properties for RAS, although further studies, including clinical evaluation, are required to confirm its overall efficacy and long-term safety. Full article

Candida infections pose a significant health threat, and conventional antifungal drugs like nystatin are limited due to poor solubility, skin permeability, and frequent dosage requirements. Nystatin effectively targets Candida species by disrupting cell membranes, but formulation issues hinder clinical use. Lipid-based vesicular carriers, or novasomes, provide controlled, prolonged drug release and enhanced skin penetration. This study focuses on developing nystatin-loaded novasomal gels as an advanced drug delivery system to enhance therapeutic efficacy, bioavailability, and patient compliance. The formulation was prepared using a modified ethanol injection technique, combining stearic acid, oleic acid, Span 60, cholesterol, and Carbopol to produce a stable transdermal gel. Comprehensive in vitro characterization using FTIR, SEM, XRD, and thermal analysis confirmed the chemical compatibility, morphological uniformity, and physical stability of the nystatin-loaded novasomal gel. Entrapment efficiency differed significantly among the formulations (p < 0.05), with F7 achieving the highest value (80%). All formulations maintained pH levels within the skin-friendly range of 5.5 to 7.0. Viscosity measurements, ranging from 3900 ± 110 to 4510 ± 105 cP, confirmed their appropriate consistency for dermal use. Rheological analysis showed a dominant elastic response, as indicated by storage modulus values consistently higher than the loss modulus. Particle size ranged from 4143 to 9570 nm, while PDI values remained below 0.3, reflecting uniform particle distribution. Zeta potential values were strongly negative, supporting physical stability. XRD studies indicated reduced crystallinity of nystatin within the formulations, while FTIR confirmed drug-excipient compatibility. SEM images showed spherical particles within the micrometer range. In vitro release studies demonstrated sustained drug release over 12 h, with F6 releasing the highest amount. The novasomal gel formulations-maintained stability for 30 days, with no notable alterations in pH, viscosity, or entrapment efficiency. Antifungal evaluation showed a larger inhibition zone (23 ± 2 mm) compared with the plain drug solution (15 ± 1.6 mm), while the MIC value was reduced (4.57 µg/mL), indicating greater potency. Skin irritation assessment in rats revealed only minor, temporary erythema, and the calculated Primary Irritation Index (0.22) confirmed a non-irritant profile. These findings suggest that the developed novasomal gel offers a promising approach for enhancing the treatment of fungal infections by enabling prolonged drug release, minimizing dosing frequency, and improving patient compliance. Full article

Tooth whitening is increasingly sought in both clinical and home settings, raising concerns about the efficacy and safety of various whitening agents and their delivery systems. This narrative review compares the whitening performance and biocompatibility of active ingredients, including hydrogen peroxide, carbamide peroxide, activated charcoal, sodium bicarbonate, fluoride compounds, and blue covarine, with particular emphasis on the role of polymer-based carriers in formulation strategies. Hydrogen peroxide and carbamide peroxide remain the most effective agents for intrinsic whitening, but are associated with risks of enamel surface alterations, microhardness reduction, and potential cytotoxicity, particularly at higher concentrations. Sodium bicarbonate provides moderate whitening effects through extrinsic stain removal, while fluoride compounds play a supportive role by reducing demineralization and tooth sensitivity, thereby preserving enamel integrity. These properties make them valuable adjuncts or alternatives for patients with high sensitivity risks. Blue covarine offers immediate optical effects without inducing intrinsic color changes, whereas activated charcoal poses risks of enamel abrasion and surface roughness with limited long-term efficacy. Polymer-based carriers such as Carbopol gels, polyvinylpyrrolidone, and hydroxypropyl methylcellulose are incorporated into whitening formulations to improve viscosity, adhesion, and modulate the release of active ingredients. These polymers might help minimize diffusion of bleaching agents into deeper dental tissues, potentially reducing cytotoxic effects, and may improve handling characteristics. However, dedicated studies evaluating the unique advantages of polymers in different whitening systems remain limited. A comprehensive understanding of both the active ingredients and delivery technologies is critical to balancing esthetic outcomes with long-term oral health. From a clinical perspective, polymer-based carriers might contribute to reducing whitening-related tooth sensitivity, improving patient comfort, and providing more predictable treatment outcomes. Continued research is needed to clarify optimal formulations and application protocols, ensuring safer and more effective tooth-whitening practices in both clinical and home-use scenarios. Full article

Background: Skin mycoses affect approximately 10% of the global population, and the range of effective topical antifungal agents remains limited. Voriconazole (VRC) is a broad-spectrum triazole with proven efficacy against drug-resistant fungal infections. This study aimed to develop and optimize VRC-loaded microemulsion (ME) polymer gels (Carbopol^®-based) for cutaneous delivery. Selected formulations also contained menthol (2%) as a penetration enhancer and potential synergistic antifungal agent. Methods: A comprehensive screening was performed using pseudoternary phase diagrams to identify stable oil/surfactant/co-surfactant/water systems. Selected MEs were prepared with triacetin, Etocas™ 35, and Transcutol^®, then gelled with Carbopol^®. Formulations were characterized for pH, droplet size, polydispersity index (PDI), and viscosity. In vitro VRC release was assessed using diffusion cells, while ex vivo permeation and skin deposition studies were conducted on full-thickness human skin. Rheological behavior (flow curves, yield stress) and texture (spreadability) were evaluated. Antifungal activity was tested against standard strain of Candida albicans and clinical isolates including a fluconazole-resistant strain. Results: The optimized ME (pH ≈ 5.2; droplet size ≈ 2.8 nm) was clear and stable with both VRC and menthol. Gelation produced non-Newtonian, shear-thinning hydrogels with low thixotropy, favorable for topical application. In ex vivo studies, performed with human skin, both VRC-loaded gels deposited the drug in the epidermis and dermis, with no detectable amounts in the receptor phase after 24 h, indicating retention within the skin. Menthol increased VRC deposition. Antifungal testing showed that VRC-containing gels produced large inhibition zones against C. albicans, including the resistant isolate. The VRC–menthol gel exhibited significantly greater inhibition zones than the VRC-only gel, confirming synergistic activity. Conclusions: ME-based hydrogels effectively delivered VRC into the skin. Menthol enhanced drug deposition and demonstrated synergistic antifungal activity with voriconazole. Full article

This study aimed to develop and characterise novel hydrogels based on natural bioactive compounds for topical antimicrobial applications. Four gel systems were formulated using different polymers, namely polyacrylic acid (Carbopol 940, CBP-G), chitosan with high and medium molecular weights (CTH-G and CTM-G), and sodium alginate (ALG-G), incorporating tinctures of Verbena officinalis and Aloysia triphylla, Laurus nobilis essential oil, and a β-cyclodextrin–clove essential oil complex. All gels displayed a homogeneous macroscopic appearance and maintained stability for over 90 days. Rheological studies demonstrated gel-like behaviour for CBP-G and ALG-G, with well-defined linear viscoelastic regions and distinct yield points, while CTM-G exhibited viscoelastic liquid-like properties. SEM imaging confirmed uniform and continuous matrices, supporting controlled active compound distribution. Thermogravimetric analysis (TG-DTA) revealed a two-step degradation profile for all gels, characterised by high thermal stability up to 230 °C and near-total decomposition by 500 °C. FTIR spectra confirmed the incorporation of bioactive compounds and products and highlighted varying interaction strengths with polymer matrices, which were stronger in CBP-G and CTH-G. Antimicrobial evaluation demonstrated that chitosan-based gels exhibited the most potent inhibitory and antibiofilm effects (MIC = 2.34 mg/mL) and a cytocompatibility assessment on HaCaT keratinocytes showed enhanced cell viability for chitosan gels and dose-dependent cytotoxicity for alginate formulations at high concentrations. Overall, chitosan-based gels displayed the most favourable combination of stability, antimicrobial activity, and biocompatibility, suggesting their potential for topical pharmaceutical use. Full article

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

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: 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