Search Results (81)

Nutritionally crucial unsaturated fatty acids, especially rich in high omega-3 bonds, are very prone to oxidation. This phenomenon makes oxidation stability a substantial challenge in every formulation, especially those which contain or at some stage of preparation contain water. Bigels and emulgels, which represent promising structured lipid systems for replacing saturated and trans fats in food formulations, pose significant oxidative stability challenges. This review examines oxidation mechanisms in such biphasic systems. Oxidation in bigels and emulgels proceeds through both free-radical-mediated autoxidation and metal-ion-catalysed pathways, with the oil–water interface serving as the primary reaction zone where pro-oxidants concentrate, and lipid substrates become accessible. Structural configuration critically determines oxidative stability, following the sequence W/O bigel > bicontinuous bigel > O/W bigel. The high viscosity of gel matrices provides substantial protection by restricting radical mobility and oxygen diffusion. Mass transfer occurs via diffusion, collision–exchange–separation, and micelle-assisted mechanisms, with association colloids forming localized interfaces that accelerate oxidation. Thermal processing presents particular challenges, as temperatures above 50 °C disrupt most gel structures and accelerate oxidative degradation. Effective protective strategies include interfacial engineering with emulsifiers to reduce oil–water interfacial tension, incorporation of natural antioxidants (e.g., phenolic compounds and tocopherols), and synergistic antioxidant combinations. This review provides a mechanistic framework for formulating oxidatively stable bigels and emulgels suitable for food applications. Full article

Phlomis L., with more than 100 species belonging to the Lamiaceae family, is a genus encompassing a diverse group of plants known for their rich phytochemical profiles and important medicinal properties. Phlomis kurdica Rech. fil. is a member of this genus widely distributed in the Middle East, especially in Iran, Iraq and Türkiye. In traditional medicine, Phlomis species have been employed in the treatment of various disorders, particularly skin conditions such as wound healing, as well as diabetes, hemorrhoids, inflammation, and gastric ulcers. The purpose of this study was to investigate the biological activities of Phlomis kurdica on skin-related enzymes and to evaluate its phytochemical properties using HPTLC, LC-MS/MS. Additionally, an emulgel formulation was developed with methanolic extract of the plant and characterized in terms of spreadability, textural profile analysis, pH, viscosity, and content quantification determination. In vitro release and rheology studies were carried out following the characterization investigations. According to our investigations, P. kurdica may be a useful component of wrinkle prevention and skin-regenerating products. Full article

Background: Human cutaneous reactivity exhibits marked inter-individual variability, yet the contribution of constitutional pigmentation traits to short-term skin responses remains incompletely characterized. Fitzpatrick skin phototype reflects stable differences in pigmentation-related traits and may therefore act as a phenotypic modifier of early cutaneous reactivity following topical exposure. Methods: In this controlled human study, 239 healthy volunteers were stratified by Fitzpatrick skin phototype into three groups: I–II (n = 138), III (n = 72), and IV–V (n = 29). A standardized emulgel-based topical provocation model was applied under occlusion to the volar forearm, and cutaneous responses were assessed at 20 min (Test A), 24 h (Test B), and 96 h (Test C) using standardized visual scoring. Group comparisons, multivariable linear regression models adjusted for age, sex, country of origin, and experimental lot, and stratified analyses by country of origin, were performed. Results: Early and short-term cutaneous responses differed significantly across phototype groups. Participants with phototypes I–II exhibited higher response scores at both 20 min and 24 h compared with phototype III (p < 0.001). In adjusted models, phototype III remained independently associated with significantly lower reactivity relative to phototypes I–II at 20 min (β = −1.61, p < 0.001) and 24 h (β = −0.98, p < 0.001). Responses among phototypes IV–V were minimal to absent; however, this subgroup was underrepresented, and findings for IV–V are descriptive. Age was a significant positive predictor of response intensity, whereas sex showed no independent association. No persistent reactions were observed at 96 h in any phototype group. Stratified analyses confirmed that the reduced reactivity associated with phototype III was independent of country of origin. Conclusions: Fitzpatrick skin phototype is independently associated with early and short-term cutaneous reactivity following standardized topical provocation in humans. Lighter phototypes (I–II) demonstrate increased susceptibility to transient inflammatory responses, whereas phototype III shows markedly reduced reactivity. These findings support the role of skin phototype as a constitutional modifier of short-term cutaneous responses and highlight the importance of considering pigmentation-related phenotypes in the design and interpretation of dermatological testing, cosmetic tolerability studies, and safety assessments of topical formulations. Full article

Ophthalmic drug delivery encounters unique challenges due to the anatomical and physiological ocular barriers, necessitating the development of novel drug delivery systems (NDDSs). This review focuses on emerging therapeutic platforms, including nanoemulsions (NEs), microemulsions (MEs), self-emulsifying drug delivery systems (SEDDSs) such as self-nano emulsifying drug delivery systems (SNEDDSs) and self-micro emulsifying drug delivery systems (SMEDDSs), emulgels, and in situ-forming emulgels, as novel strategies for enhancing ocular drug delivery. NEs and MEs, due to their small globule size, excellent drug solubility, stability, and bioavailability, offer promising solutions for effective ocular therapy. SEDDSs further enhance the stability and bioavailability of hydrophobic drugs through self-emulsification in aqueous environments. Emulgels, combining the benefits of emulsions and gels, provide sustained and controlled release of therapeutic agents, improving the ocular retention time and therapeutic efficacy. Additionally, in situ-forming emulgels offer the advantage of liquid-to-gel transition upon contact with ocular surfaces, optimizing drug delivery. The review discusses various ocular diseases, challenges for ocular delivery of conventional formulations, updates on emulsion-based novel drug delivery systems for ophthalmic drug delivery, mechanisms of enhanced ocular permeation, formulation strategies, advantages, and challenges, design-of-experiment considerations for optimization, characterizations, and recent advancements in these systems including patents and clinical trials, highlighting their potential for improving the treatment of various ocular diseases. Furthermore, this review explores marketed ophthalmic emulsions and future prospects for integrating these NDDSs into clinical ophthalmology, emphasizing their ability to overcome ocular barriers and enhance therapeutic efficacy. Full article

Background: Natural alternatives are becoming more popular as a result of health risks associated with synthetic preservatives in pharmaceuticals. Because of its antibacterial properties, Psidium guajava (L.) leaf extract is a practical choice for sustainable preservation. Objectives: The aim of this research is to evaluate the efficacy of Psidium guajava (L.) leaf extract as a 10% (w/w) natural preservative in five different base formulations: creams (clotrimazole cream, permethrin cream, and gentamicin cream) and gels (indomethacin emulgel and ibuprofen gel). Methods: Over the course of 28 days, antimicrobial activity against Pseudomonas aeruginosa, Staphylococcus aureus, Escherichia coli, Aspergillus brasiliensis, and Candida albicans was evaluated. In accordance with USP/BP guidelines, three months of accelerated conditions (40 ± 2 °C/75% ± 5% RH) were used to assess chemical, physical, and microbiological stability. The stability of the active component was examined using HPLC. Results: Our findings showed that the extract completely inhibited the growth of tested bacterial species in clotrimazole cream, permethrin cream, gentamicin cream, and indomethacin emulgel, demonstrating significant antibacterial activity across all formulations. However, the antifungal activity was restricted. The preservation effectiveness criterion (bacterial/yeast counts < 10 CFU, mold < 20 CFU) was only fulfilled by ibuprofen gel and clotrimazole cream. Although there were color changes, stability tests verified that the active components such as ibuprofen (reduced from 97.5% to 92%) and clotrimazole (reduced from 99.9% to 95%) decomposed minimally and had acceptable physical characteristics. Particularly against fungus, the extract was surpassed by chemical preservatives (methyl/propyl paraben). Conclusions: Certain semi-solid pharmaceuticals can benefit from the stability and antimicrobial protection provided by guava leaf extract, a natural preservative. The weak antifungal activity of the guava leaf extract emphasizes the necessity for specific improvements in the formulation. Full article

Background: The treatment of bacterial dermatological diseases is currently facing major difficulties, determined by the alarming increase in the resistance of pathogenic bacteria to conventional therapies. In this context, a viable and effective alternative is represented by the use of phytocompounds to obtain the desired therapeutic effect. The essential oil of Origanum vulgare L. stands out for its antibacterial, anti-aging, collagen synthesis stimulating and wound healing properties. However, its use is limited by certain disadvantages, such as poor stability and the risk of skin irritation due to accumulation in the dermis. Method: The process of formulating the emulgel with oregano oil respected the specific technological steps. The resulting emulgel was subjected to a series of tests, including organoleptic, stability and antimicrobial efficacy determinations. In addition, an in vivo study was conducted to confirm the lack of irritation, involving six groups of patients differentiated by age, sex and skin phenotype. Results: The test results revealed that the emulgel formulated with oregano oil is stable, has organoleptic properties and an appropriate pH for topical use. The product demonstrated antibacterial efficacy against Staphylococcus aureus and Pseudomonas aeruginosa. In addition, short-term in vivo tests (20 min—96 h) confirmed the safety and absence of skin irritation, indicating its potential as an effective alternative treatment. Conclusions: In conclusion, the emulgel with origanum oil represents an innovative formulation for topical application. The product is well tolerated by the skin and does not cause irritation, and its antibacterial properties validate it as a promising therapeutic solution. Full article

Background/Objectives: Breast cancer remains the most prevalent malignancy among women worldwide, with letrozole (LZ) serving as a critical aromatase inhibitor for hormone receptor–positive cases. However, long-term oral administration of LZ is often associated with systemic adverse effects and poor patient compliance. To overcome these limitations, new non-aqueous nanoemulgels (NEMGs) were developed for transdermal delivery of LZ. Methods: The NEMGs were formulated using glyceryl monooleate (GMO), Sepineo P600^®, Transcutol, propylene glycol, and penetration enhancers propylene glycol laurate (PGL), propylene glycol monocaprylate (PGMC), and Captex^®. Physicochemical characterization, solubility, stability, and in vitro permeation studies were conducted using Strat-M^® membranes, while in vivo pharmacokinetics were evaluated in rat models. Results: The optimized GMO/PGMC-based NEMG demonstrated significantly enhanced drug flux, higher permeability coefficients, and shorter lag times compared with other NEMGs and suspension emulgels. In vivo, transdermal application of the GMO/PGMC-based NEMG over an area of 2.55 cm² produced dual plasma absorption peaks, with 57% of the LZ dose absorbed relative to oral administration over 12 days. Shelf-life and accelerated stability assessments confirmed excellent physicochemical stability with negligible crystallization. Conclusions: The developed LZ NEMG formulations offer a stable, effective, and patient-friendly transdermal drug delivery platform for breast cancer therapy. This system demonstrates potential to improve patient compliance and reduce systemic toxicity compared to conventional oral administration. Full article

Cosmeceutical systems represent next-generation topical platforms designed to deliver bioactive molecules with therapeutic potential directly to the skin. This study evaluated four anti-wrinkle formulations (three creams and one emulgel) in terms of their stability, sensory characteristics, acceptability, and skin tolerance. The products incorporated a unique combination of active ingredients, including N-acetylcysteine, arginine HCl, Blainvillea camellia flower extract, tocopherol, and hyaluronic acid. For the cream formulations (EG01–EG03), different emulsifiers were employed, while EG04 was developed as an emulgel. Stability testing revealed that only three out of four formulations remained physically stable, with EG04 showing phase separation. Sensory analysis assessed parameters such as spreading, absorption, shininess, stickiness, greasiness, and smoothness, with results illustrated using a radar plot. EG01 and EG03 displayed similar sensory profiles, differing mainly in shininess and greasiness, while both exhibited high smoothness. In vivo testing was conducted on female human volunteers aged 50–65 years (Fitzpatrick skin types II–IV) to evaluate tolerance and acceptability. Only EG01 and EG03, formulated with methyl glucose sesquistearate and polyglyceryl-3-methylglucose distearate, respectively, demonstrated both superior sensory performance and 100% acceptability and tolerance in clinical assessment. Full article

Equisetum telmateia Ehrh. (great horsetail) belongs to the Equisetaceae family and its aerial parts have been traditionally used for skin conditions and to achieve healthy and resilient skin, nails, and hair. This study aimed to evaluate the inhibition of skin-related enzymes by, the antioxidant capacity of, and the phytochemical composition of E. telmateia. Additionally, a novel emulgel was formulated from the main methanolic extract and characterized in terms of pH, viscosity, determination of content quantification, textural profile analysis, and spreadability. After the characterization studies, in vitro release and ex vivo permeation and penetration studies were performed. Firstly, the dried aerial parts of E. telmateia were macerated in methanol, followed by partitioning with solvents of increasing polarity: n-hexane, chloroform, ethyl acetate, and n-butanol. Antioxidant activity was assessed using DPPH, FRAP, CUPRAC, and TOAC assays, while enzyme inhibition was analyzed for collagenase, elastase, hyaluronidase, and tyrosinase. LC-MS/MS analysis identified 53 phytochemical compounds. Protocatechuic acid, the main phenolic compound, was quantitatively analyzed in each subfraction by HPTLC. The in vitro release studies showed sustained release of the reference substance (protocatechuic acid) and the kinetic modeling of the release was fitted to the Higuchi model. The ex vivo permeation and penetration studies showed that the formulation exhibited a retention of 3.06 ± 0.21 µg.cm⁻² after 24 h, whereas the suspended extract demonstrated a skin retention of 1.28 ± 0.47 µg.cm⁻². Both the extracts and the formulated emulgel exhibited inhibitory effects on skin-related enzymes. Our finding suggested that E. telmateia might be a valuable ingredient for wrinkle care and skin-regenerating cosmetics. Full article

Meloxicam is a promising non-steroidal anti-inflammatory drug (NSAID) for acute and chronic pain prevention and treatment. Due to its poor water solubility, the clinical use of meloxicam is limited. In addition, for transdermal applications, the impermeability of the skin makes it difficult to conceive an appropriate NSAID-based delivery system that can penetrate through the skin barrier. Hydrophilic/hydrophobic gels, designed as transdermal drug delivery systems, can considerably improve other drug administration types (such as oral or intravenous), avoiding or limiting the side effects. The main purpose of this paper is to present some physicochemical and pharmaceutical considerations about meloxicam and to review the most important research concerning the gels used for the transdermal delivery of meloxicam. Thus, smart polymeric networks, semi-solid systems (lipogels, emulgels), β-cyclodextrin-based gels, liposomes (ethosomes, niosomes, flexosomes, transferosomes, menthosomes, invasomes), and nanostructured lipid carriers, with analgesic and anti-inflammatory activity, are discussed. The key objective of this study was to highlight various gel formulations with enhanced properties, which could be used in a minimally invasive manner for the sustained administration of meloxicam. Full article

Hydrogels (Hy) were obtained with a ternary system of proteins (pea (P) or soy isolate (S) 2%), guar (0.5%), and xanthan gums (0.5%) and were subjected to thermal treatment (70 °C/20 min or 85 °C/15 min, or not) prior to structure formation. The FTIR spectra of the hydrogels and the turbidity test (spectrophotometrically red at 600 nm) were used for studying protein–polysaccharide interactions. Amplitude sweeps (0.01–100%) and flow behavior tests (0.1–100 s⁻¹) were conducted for structure analysis. Emulgels were obtained by emulsification of the Hy with 40% or 60% sunflower oil. The centrifugal stability and texture (TPA test) of the emulgels were assessed and SND_40% exhibited the highest hardness (5.30 ± 0.23 N). Based on the results, SND_40%, PND_40%, SD70_40%, and PD_70% were chosen as fat-replacing systems in biscuit formulation. The textural, color, and stability attributes of the reformulated samples were compared with a reference containing margarine. Increased hardness and fracturability were determined for the emulgel-based biscuits, while the color parameters were statistically similar to the reference. Thermal treatments applied to enhance protein–polysaccharide interactions increased the structural performances of some emulgels, while their application as fat-replacing systems should be further evaluated since no statistical differences were recorded in the sensory evaluation of the reference and reformulated biscuits. Emulgels with tuned technological properties have the potential to replace saturated fats in foods. 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

Periodontitis is a prevalent oral condition worldwide. Azithromycin, a conventional lipophilic drug for periodontal treatment, often causes systemic side effects when administered orally. To address this, azithromycin-loaded nano-emulgels were developed using olive oil as a carrier within a xanthan gum aqueous gel phase. This oil-in-aqueous gel emulsion was actuated into a foam for localized drug delivery in gingival and periodontal disease. The solubility of azithromycin in various vehicles was tested, with olive oil showing the best solubility (0.347 mg/mL). Thermodynamic stability testing identified viable nano-formulations, with encapsulation efficiencies ranging from 98 to 100%. These formulations exhibited rapid drug release within 2–8 h. Muco-adhesion studies and ex vivo permeability tests on porcine buccal mucosa highlighted the beneficial properties of xanthan gum for local drug retention within the oral cavity. Antimicrobial efficiency was assessed using minimum inhibitory concentrations against various oral pathogens, where the formulation with equal surfactant and co-surfactant ratios showed the most potent antibacterial activity, ranging from 0.390 to 1.56 µg/mL. This was supported by the shear-thinning, muco-adhesive, and drug-retentive properties of the xanthan gel base. The study also examined the influence of the oil phase with xanthan gum gel on foam texture, rheology, and stability, demonstrating a promising prototype for periodontitis treatment. Full article

This study explores the eco-friendly extraction and formulation of emulgels based on Black Sea shark liver oil for their potential anti-inflammatory and wound healing dermatocosmetic applications. Two emulgel formulations were prepared: Gel 1, containing shark liver oil, and Gel 2, combining shark liver oil with borage oil. The eco-friendly extraction of shark liver oil was performed, yielding a high content of polyunsaturated omega-3 fatty acids, primarily eicosapentaenoic acid (16.68 ± 0.28 mg/g %) and docosahexaenoic acid (18.14 ± 0.31 mg/g %). Physicochemical evaluations of the emulgels revealed excellent stability over time, with small variations in pH, viscosity, and spreadability, confirming their robustness. Rheological analysis demonstrated pseudoplastic behavior for both formulations, with Gel 2 exhibiting a more favorable flow and consistency index (K = 34.11, n = 0.28) compared to Gel 1 (K = 32.73, n = 0.29). The anti-inflammatory effect was evaluated using two experimental edema models: 10% kaolin suspension and 6% dextran solution. Both emulgels demonstrated significant edema reduction, with Gel 2 showing a more potent anti-inflammatory effect. The wound healing effect was assessed in vivo, revealing that Gel 2 accelerated wound closure and hair restoration, outperforming Gel 1 and the reference diclofenac gel. These results suggest that Black Sea shark liver oil-based emulgels, especially borage oil formulation, offer promising eco-friendly alternatives for dermatocosmetic applications, with enhanced anti-inflammatory and wound healing properties. Full article