Innovative Alkanediol-Based Eutectic Solvents for Extracting/Pre-Formulating Dermatologically Valuable Free Fatty Acids from Spirulina and Porphyridium Cakes.

The growing demand for phycobiliproteins from microalgae generates a significant volume of by-products, such as extraction cakes. These cakes are enriched with products of interest for the cosmetics market, namely free fatty acids, particularly polyunsaturated (PUFA). In this work, two cakes, one of spirulina and one of Porphyridium cruentum, were valorized using innovative natural hydrophobic deep eutectic solvents (NaDES) based on alkanediols. The most promising NaDES, as determined by physicochemical properties and screening, are mixtures of alkanediols and fatty acids. These include the mixtures of 1,3-propanediol and octanoic acid (1:5, mol/mol) and 1,3-propanediol and octanoic and decanoic acid (1:3:1, mol/mol). Two extractive processes were implemented: ultrasound-assisted extraction and an innovative mechanical process involving dual asymmetric centrifugation. The second process resulted in the production of extracts significantly enriched in PUFA, ranging from 65 to 220 mg/g dry matter with the two cakes. The extracts and NaDES demonstrated good safety with respect to epidermal keratinocyte viability (>80% at 200 µg/mL). The study of their impact on commensal and pathogenic cutaneous bacteria demonstrated significant effects on the viability of Staphylococcus aureus and Staphylococcus epidermidis (>50% decrease at 200 µg/mL) while preserving Corynebacterium xerosis and Cutibacterium acnes. These results highlight the potential of valorizing these co-products using alkanediol-based NaDES, in a strategy combining an active vector (NaDES) and a growth regulator extract, for the management of cutaneous dysbiosis involving staphylococci.

Recent advances of electrospun strategies in topical products encompassing skincare and dermatological treatments.

As the potential applications of electrospinning in healthcare continue to be explored, along with advancements in industrial-scale solutions and the emergence of portable electrospinning devices, some researchers have explored electrospinning technology in topical products, including its application in skincare, such as facial masks, beauty patches, sunscreen, and dermatological treatments for conditions like atopic dermatitis, psoriasis, acne, skin cancer, etc. In this review, we first outline the fundamental principles of electrospinning and provide an overview of existing solutions for large-scale production and the components and functionalities of portable spinning devices. Based on the essential functionalities required for skincare products and the mechanisms and treatment methods for the aforementioned dermatological diseases, we summarize the potential advantages of electrospinning technology in these areas, including encapsulation, sustained release, large surface area, and biocompatibility, among others. Furthermore, considering the further commercialization and clinical development of electrospinning technology, we offer our insights on current challenges and future perspectives in these areas, including issues such as ingredients, functionality, residue concerns, environmental impact, and efficiency issues.

Influence of type of vehicle on dermal penetration efficacy of hydrophilic, amphiphilic, lipophilic model drugs.

The influence of the vehicle on the dermal penetration efficacy of three different active ingredient (AI) surrogates (hydrophilic, amphiphilic, lipophilic model drugs), that were incorporated into these vehicles, was investigated with the ex vivo porcine ear model, which allowed to assess time and space resolved dermal penetration profiles of the AI. Fifteen different vehicles, including classical vehicles (hydrogel, oleogel, o/w cream, w/o ointment, amphiphilic cream) and innovative vehicles were included into the study. Results show tremendous differences in the penetration efficacy of the AI among the different vehicles. The differences in the total amounts of penetrated AI between lowest and highest penetration were about 3-fold for the hydrophilic AI surrogate, 3.5-fold for the amphiphilic AI and almost 5-fold for the lipophilic AI. The penetration depth was also affected by the type of vehicle. Some vehicles allowed the AI to penetrate only into the upper layers of the stratum corneum, whereas others allowed the penetration of the AI into deeper layers of the viable dermis. Data therefore demonstrate that the vehicles in compounding medications cannot be exchanged against each other randomly if a constant and safe medication is desired. The data obtained in the study provide first information on which types of vehicles are exchangeable and which types of vehicles can be used for enhanced dermal penetration of AI, thus providing a first base for a science-based selection of vehicles that can provide both, efficient dermal drug delivery and skin barrier function maintenance/strengthening at the same time.

Locally acting dermatology drug products: Pharmaco-analytic considerations for bioequivalence.

Bioequivalence determinations for locally acting dermatology drug products rely on assessing product sameness thru physicochemical composition and structure comparison, comparing the concentration of the active ingredient at the putative site of action, or comparing the clinical performance of the test (would-be generic) and reference products. Topical product action on cutaneous disease may be confounded by the action of excipients and are also subject to the inherent variability of how product may interact with the skin, including thermodynamic factors such as evaporation, spreadability, and interaction with the local environment such as heat and light and skin moisture.

Recent Advancements and Trends of Topical Drug Delivery Systems in Psoriasis: A Review and Bibliometric Analysis.

Psoriasis is an immune-mediated inflammatory skin disease where topical therapy is crucial. While various dosage forms have enhanced the efficacy of current treatments, their limited permeability and lack of targeted delivery to the dermis and epidermis remain challenges. We reviewed the evolution of topical therapies for psoriasis and conducted a bibliometric analysis from 1993 to 2023 using a predictive linear regression model. This included a comprehensive statistical and visual evaluation of each model's validity, literature profiles, citation patterns, and collaborations, assessing R variance and mean squared error (MSE). Furthermore, we detailed the structural features and penetration pathways of emerging drug delivery systems for topical treatment, such as lipid-based, polymer-based, metallic nanocarriers, and nanocrystals, highlighting their advantages. This systematic overview indicates that future research should focus on developing novel drug delivery systems characterized by enhanced stability, biocompatibility, and drug-carrying capacity.

Development of a film-forming oleogel with increased substantivity for the treatment of psoriasis.

The aim of this work was the development of a film-forming formulation (FFF) for the topical treatment of psoriasis that shows an increased substantivity compared to conventional semi-solid dosage forms. The developed formulation is an oleogel. It is based on a combination of castor oil and medium chain triglycerides, and the oil-soluble film former MP-30 (Croda GmbH, Nettetal, Germany), a polyamide that upon mixing with a polar oil entraps the oil und thus substantially increases the viscosity of the formulation up to a semisolid state. Betamethasone dipropionate (BDP) and calcipotriole (CA) were used as active pharmaceutical ingredients (APIs). Oleogels of different compositions were evaluated regarding substantivity, rheological properties, ex-vivo penetration into the skin and ex-vivo permeation through the skin. Marketed products were used as controls. It was found that the amount of betamethasone dipropionate penetrating and permeating into and through the skin from the film-forming formulation is at an intermediate value compared to the marketed products. The substantivity of the developed formulation is described by an amount of 57.7 % formulation that remains on the skin surface and is thus significantly higher compared to the marketed products. In the film forming formulation, the proportion of API penetrating the skin remains the same when the skin repetitively brought in contact with a piece of textile during the penetration experiment. In contrast with the in-market formulations tested, this proportion was reduced by up to 97 %. As a result, the developed formulations can lead to an increased patient compliance.

Formulation development of tazarotene-loaded PLGA nanoparticles for follicular delivery in the treatment of inflammatory skin diseases.

Tazarotene is a widely prescribed topical retinoid for acne vulgaris and plaque psoriasis and is associated with skin irritation, dryness, flaking, and photosensitivity. In vitro permeation of tazarotene was studied across the dermatomed human and full-thickness porcine skin. The conversion of tazarotene to the active form tazarotenic acid was studied in various skin models. Tazarotene-loaded PLGA nanoparticles were prepared using the nanoprecipitation technique to target skin and hair follicles effectively. The effect of formulation and processing variables on nanoparticle properties, such as particle size and drug loading, was investigated. The optimized nanoparticle batches with particle size <500 µm were characterized further for FT-IR analysis, which indicated no interactions between tazarotene and PLGA. Scanning electron microscopy analysis showed uniform, spherical, and non-agglomerated nanoparticles. In vitro release study using a dialysis membrane indicated a sustained release of 40-70 % for different batches over 36 h, following a diffusion-based release mechanism based on the Higuchi model. In vitro permeation testing (IVPT) in full-thickness porcine skin showed significantly enhanced follicular and skin delivery from nanoparticles compared to solution. The presence of tazarotenic acid in the skin from tazarotene nanoparticles indicated the effectiveness of nanoparticle formulations in retaining bioconversion ability and targeting follicular delivery.

Screening of avocado oil nanoformulations intended to skin delivery / Análisis de nanoformulaciones de aceite de aguacate para aplicación cutánea

INTRODUCTION: vegetable ingredients are increasingly common in skin products. Avocado oil is an ingredient of natu¬ral sources with various properties on the skin. In this work, crude avocado oil-loaded nanocapsules were evaluated regarding its physicochemical stability to obtain a formulation of skin delivery with adequate quality: suitable physi¬cochemical stability, with low polydispersity and with a pH suitable for cutaneous application. METHOD: nanoparticle formulations with components variation were evaluated for 2 months. Nanoparticle formu¬lation considered the most stable was further evaluated for 6 months. Furthermore, the oxidative stability of crude avocado oil loaded in nanocapsules and standard avocado oil was also performed to detect any sign of oil oxidation. RESULTS: all formulations had negative zeta potential after 2 months of storage. pH values of nanoparticles remained stable throughout the test. Formulation with the lowest content of ingredients exhibited the highest stability after 2 months of storage. Nanoencapsulated avocado oil and crude avocado oil showed no evidence of oxidation. CONCLUSIONS: Aqueous dispersions with the lowest content of ingredients presented the best physicochemical sta¬bility. Therefore, we have demonstrated preliminary the feasibility of developing avocado-oil loaded nanocapsules

INTRODUCCIÓN: los ingredientes vegetales son cada vez más comunes en los productos para la piel. El aceite de aguacate es un ingrediente de origen natural con varias propiedades en la piel. En este trabajo se evaluó la estabilidad físico-química de las nanocápsulas cargadas con aceite de aguacate crudo para obtener una formulación de aplicación cutánea con calidad adecuada: estabilidad físico química adecuada, con baja polidispersidad y con pH adecuado para aplicación cutánea. MÉTODO: formulaciones de nanocápsulas con variación en la composición de los ingredientes fueron evaluadas durante 2 meses. La formulación de nanocápsulas considerada más estable se evaluó por 6 meses. Además, la estabilidad oxidativa del aceite de aguacate de las nanocápsulas y del aceite de aguacate estándar también fue evaluada para detectar cualquier signo de oxidación. RESULTADOS: todas las formulaciones han tenido potencial zeta negativo después de 2 meses de almacenamiento. Los valores de pH de las nanopartículas se mantuvieron estables durante toda la prueba. La formulación con el contenido más bajo de ingredientes exhibió la mayor estabilidad después de 2 meses de almacenamiento. El análisis de aceite de aguacate crudo y del aceite de aguacate nanoencapsulado no mostró evidencia de oxidación. CONCLUSIONES: la dispersión acuosa con el contenido más bajo de ingredientes presentó la mejor estabilidad fisicoquímica. Además, el aceite de aguacate no ha mostrado evidencia de oxidación. Por lo tanto, hemos demostrado preliminarmente la viabilidad de desarrollar nanocápsulas cargadas de aceite de aguacate

A randomized half-body, double blind, controlled trial on the effects of a pH-modified moisturizer vs. standard moisturizer in mild to moderate atopic dermatitis,

Abstract Background: Higher skin pH in atopic dermatitis contributes to impaired epidermal barrier. A moisturizer compatible with physiological pH could improve atopic dermatitis. Objective: To determine the effect of a physiologically compatible pH moisturizer in atopic dermatitis. Methods: A randomized half body, double blind, controlled trial involving patients with stable atopic dermatitis was performed. pH-modified moisturizer and standard moisturizer were applied to half body for 6 weeks. Results: A total of 6 (16.7%) males and 30 (83.3%) females participated. Skin pH reductions from week 0, week 2 and 6 were significant at the forearms (5.315 [0.98] to 4.85 [0.54] to 5.04 [0.78], p = 0.02) and abdomen (5.25 [1.01], 4.82 [0.64], 5.01 [0.59], p = 0.00) but not at the shins (5.01 [0.80], 4.76 [0.49], 4.85 [0.79], p = 0.09) with pH-modified moisturizer. Transepidermal water loss (TEWL) at the forearms decreased (4.60 [2.55] to 3.70 [3.10] to 3.00 [3.55], p = 0.00), abdomen (3.90 [2.90] to 2.40 [3.45] to 2.70 [2.25], p = 0.046). SCORAD improved from 14.1 ± 12.75 to 10.5 ± 13.25 to 7 ± 12.25, p = 0.00. In standard moisturizer group, pH reductions were significant at the forearms (5.29 [0.94] to 4.84 [0.55] to 5.02 [0.70], p = 0.00) and abdomen (5.25 [1.09], 4.91 [0.63], 5.12 [0.66], p = 0.00). TEWL at the forearm were (4.80 [2.95], 4.10 [2.15], 4.60 [3.40], p = 0.67), shins (3.80 [1.40], 3.50 [2.35], 4.00 [2.50], p = 0.91) and abdomen (3.70 [2.45], 4.10 [3.60], 3.40 [2.95], p = 0.80). SCORAD improved from 14.2 ± 9.1 to 10.9 ± 10.65 to 10.5 ± 11, p = 0.00. Reduction in pH was observed with both moisturizers while TEWL significantly improved with pH-modified moisturizer. pH-modified moisturizer resulted in greater pH, TEWL and SCORAD improvements however the differences were not significant from standard moisturizer. Study limitation: Skin hydration was not evaluated. Conclusion: Moisturization is beneficial for atopic dermatitis; use of physiologically compatible pH moisturizer is promising.

Diseño y evaluación in vivo de fórmulas para acné basadas en aceites esenciales de naranja (Citrus sinensis), albahaca (Ocimum basilicum L) y ácido acético / Effectiveness of antimicrobial formulations for acne based on orange (Citrus sinensis) and sweet basil (Ocimum basilicum L) essential oils

Introducción. Actualmente, la resistencia a los antimicrobianos de las cepas bacterianas involucradas en el desarrollo del acné es una realidad y se hace necesario buscar alternativas terapéuticas para su tratamiento. Objetivos. Diseñar fórmulas en gel a base de aceites esenciales y ácido acético, y evaluar su efectividad en pacientes voluntarios afectados por acné. Materiales y métodos. Se trata de un estudio experimental simple enmascarado de tres fórmulas en gel sobre cuatro grupos de siete pacientes. Los tratamientos antibacterianos (aceites esenciales), queratolíticos y mixtos (ácido acético), se aplicaron diariamente por espacio de ocho semanas. Se hicieron controles semanales para evaluar la evolución de los pacientes. Resultados. Todos los grupos reportaron mejoría (desaparición de las lesiones) de la condición del acné, la cual osciló entre 43 y 75 %, con leves efectos secundarios transitorios relacionados con la aplicación de los tratamientos utilizados. Conclusiones. Las fórmulas estudiadas mostraron ser estables química y físicamente durante la aplicación de los tratamientos, lo cual se demostró mediante análisis de cromatografía de gases, en la cual no se evidenció ningún cambio en los perfiles de composición de los aceites esenciales ni en el del ácido acético. Los resultados se catalogaron entre buenos y excelentes, en particular, el del ácido acético, que logró mejorías superiores al 75 %, dada su actividad mixta antiséptica y queratolítica. Los efectos secundarios (ardor y enrojecimiento) desaparecieron a los pocos minutos de realizada la aplicación y no impidieron el cumplimiento de los tratamientos.

Introduction. Currently, the antimicrobial resistance has developed in bacterial strains involved in the development of acne. Therefore, alternatives to antibiotic treatment have become necessary. Objectives. Gel formulations were designed based on essential oils and acetic acid, and their effectiveness was evaluated in patients affected by acne. Materials and methods. Masked simple experimental study of three gel formulations on 28 volunteer patients, separated in four groups of seven patients. Treatments were applied daily for eight weeks and consisted of (1) antibacterial (essential oils), (2) keratolytic medication (3) essential oils mixed with acetic acetic, and (4) kerolytic medication with acetic acid. Weekly checks were conducted to evaluate patient improvement. Results. All groups reported an improvement of the acne condition, which ranged between 43% and 75% clearance of lesions. Evidence of treatment disappeared within minutes, showing little discomfort or side effects after application. Conclusions. The essential oil formulations were chemically and physically stable during application of treatments. This was demonstrated by gas chromatography, where no evidence no change neither the composition profiles of essential oils nor in acetic acid. The results were ranked good to excellent, particularly for the acetic acid mixture, which achieved improvements of 75%. This appeared to be a result of their joint antiseptic and keratolytic activity. Side effects (burning and redness) disappeared within a few minutes of completing the application, therefore, did not interfere with adherence to treatment.