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1.
J Dermatol ; 49(9): 805-817, 2022 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-35567311

RESUMEN

The coronavirus disease 2019 (COVID-19) pandemic caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) enforced the use of hand sanitation and of personal protective equipment, such as masks and visors, especially by health-care professionals, but also by the general public. However, frequent hand sanitation and the prolonged and continuous use of personal protective equipment are responsible for constant frictional and pressure forces on skin causing lesions, the most reported being acne, facial itching, dryness, and rash. Thus, it is important to find measures to prevent skin lesions, in order to improve the quality of life of health-care professionals and of the general public. This article gathers the current information regarding measures to prevent human to human transmission of COVID-19, reviews the most common skin lesions caused by the use of hand sanitizers and different types of personal protective equipment, and the possible preventive measures that can be used on a daily basis to minimize the risk of developing skin-related pathologies. Daily skin care routines and the incorporation of a dressing between the skin and the personal protective equipment to serve as a protective barrier are some of the applied measures. Moisturizers and dressings improve the skin's ability to respond to constant aggressions. Lastly, the need for additional studies to evaluate the lubrication properties of different types of dressings is discussed. The understanding of what kind of dressing is more suitable to prevent pressure injuries is crucial to promote healthy skin and wellbeing during pandemic times.


Asunto(s)
COVID-19 , Enfermedades de la Piel , COVID-19/epidemiología , COVID-19/prevención & control , Humanos , Equipo de Protección Personal/efectos adversos , Calidad de Vida , SARS-CoV-2 , Saneamiento , Enfermedades de la Piel/etiología
2.
AAPS PharmSciTech ; 23(4): 107, 2022 Apr 05.
Artículo en Inglés | MEDLINE | ID: mdl-35381882

RESUMEN

Palatability and swallowability in the pediatric population are perceived as true challenges in the oral administration of medication. Pediatric patients have high sensitivity to taste and reduced ability to take solid dosage forms, which can often lead to a poor therapeutic compliance. It is crucial to find new strategies to simplify the oral administration of drugs to children. The present paper reports the development of a new hydrogel vehicle adapted to the pediatric population. Several polymers with similar properties were selected and adjustments were made to obtain the desired characteristics of the final product. The developed formulations were studied for organoleptic properties, rheology, mucoadhesion properties, preservative efficacy, and stability. Physical and chemical compatibilities between the vehicle and several drugs/medicines, at the time of administration, were also studied. Six final formulations with different polymers, odor, and color were chosen, and no known interactions with medications were observed. The proposed new oral vehicles are the first sugar-free vehicle hydrogels designed to make the intake of oral solid forms a more pleasant and safer experience for pediatric patients.


Asunto(s)
Hidrogeles , Pediatría , Administración Oral , Niño , Excipientes , Humanos , Cooperación del Paciente
3.
J Agric Food Chem ; 70(14): 4221-4242, 2022 Apr 13.
Artículo en Inglés | MEDLINE | ID: mdl-35357173

RESUMEN

Over the years, the growth of the world population has caused a huge agricultural production to support the population's needs. Since plant protection products are essential to preserve agricultural crops and to optimize vital plant processes, it is crucial to use more sustainable, biodegradable, and biocompatible raw materials, without harming the environment and human health. Although the development of new plant protection products is a costly process, the environmental benefits should be considered. In this context, marine raw materials obtained as byproducts of fishing industries, possessing a wide variety of physicochemical and biological properties, can serve as a promising source of such materials. They have a high potential for developing alternative and safe formulations for agricultural applications, not only as biocompatible excipients but also as effective and selective, or even both. It is also possible to promote a synergistic effect between an active substance and the biological activity of the marine polymer used in the formulation, enabling plant protection products with lower concentrations of the active substances. Thus, this review addresses the repurposing of marine raw materials for the development of innovative plant protection products, focusing on micro- and nanoparticulate formulations, to protect the environment through more ecological and sustainable strategies.


Asunto(s)
Agricultura , Productos Agrícolas , Materiales Biocompatibles , Humanos , Polímeros
4.
Acta Biomater ; 142: 14-35, 2022 04 01.
Artículo en Inglés | MEDLINE | ID: mdl-35202853

RESUMEN

Hair care and treatment has evolved significantly through the years as new formulations are continuously being explored in an attempt to meet the demand in cosmetic and medicinal fields. While standard hair care procedures include hair washing, aimed at hair cleansing and maintenance, as well as hair dyeing and bleaching formulations for hair embellishment, modern hair treatments are mainly focused on circumventing hair loss conditions, strengthening hair follicle properties and treat hair infestations. In this regard, active compounds (ACs) included in hair cosmetic formulations include a vast array of hair cleansing and hair dye molecules, and typical hair treatments include anti-hair loss ACs (e.g. minoxidil and finasteride) and anti-lice ACs (e.g. permethrin). However, several challenges still persist, as conventional AC formulations exhibit sub-optimal performance and some may present toxicity issues, calling for an improved design of formulations regarding both efficacy and safety. More recently, nano-based strategies encompassing nanomaterials have emerged as promising tailored approaches to improve the performance of ACs incorporated into hair cosmetics and treatment formulations. The interest in using these nanomaterials is based on account of their ability to: (1) increase stability, safety and biocompatibility of ACs; (2) maximize hair affinity, contact and retention, acting as versatile biointerfaces; (3) enable the controlled release of ACs in both hair and scalp, serving as prolonged AC reservoirs; besides offering (4) hair follicle targeting features attending to the possibility of surface tunability. This review covers the breakthrough of nanomaterials for hair cosmetics and hair treatment, focusing on organic nanomaterials (polymer-based and lipid-based nanoparticles) and inorganic nanomaterials (nanosheets, nanotubes and inorganic nanoparticles), as well as their applications, highlighting their potential as innovative multifunctional nanomaterials towards maximized hair care and treatment. STATEMENT OF SIGNIFICANCE: This manuscript is focused on reviewing the nanotechnological strategies investigated for hair care and treatment so far. While conventional formulations exhibit sub-optimal performance and some may present toxicity issues, the selection of improved and suitable nanodelivery systems is of utmost relevance to ensure a proper active ingredient release in both hair and scalp, maximize hair affinity, contact and retention, and provide hair follicle targeting features, warranting stability, efficacy and safety. This innovative manuscript highlights the advantages of nanotechnology-based approaches, particularly as tunable and versatile biointerfaces, and their applications as innovative multifunctional nanomaterials towards maximized hair care and treatment.


Asunto(s)
Cosméticos , Preparaciones para el Cabello , Nanoestructuras , Cabello , Preparaciones para el Cabello/farmacología , Nanotecnología
5.
J Cosmet Dermatol ; 21(2): 513-529, 2022 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-34871468

RESUMEN

INTRODUCTION: Currently, the demand for the use of constituents of natural origin in cosmetic formulations in detriment of synthetic compounds is noticeable. Several studies assess the potential of essential oils when incorporated into various cosmetic formulations and study their biological activities. This work intends to prepare a literature review on essential oils tested in dermocosmetic formulations and whose biological activities were evaluated through in vitro and/or in vivo tests. The main objectives for this study were as follows: to identify the essential oils that have been used in cosmetic formulations; and compile information on the main biological activities tested in cosmetic formulations. METHODS: A search was carried out until 2021 in the scientific databases PubMed and Web of Science, using different search terms, and several scientific articles from in vitro and in vivo studies in animals and clinical trials were selected and analyzed of involving development dermocosmetic formulations containing essential oils and the analysis of their biological activities. RESULTS: These studies demonstrate that the antimicrobial activity (antibacterial and antifungal) is the one most studied, mainly through in vitro tests. In vivo studies were also carried out either in animals or in clinical studies showing different effects, such as repellent action, inhibition of hair growth, and action against migraine. Regarding formulations, it was evident that creams are the most used. CONCLUSIONS: There is enormous potential for the use of essential oils in future formulations in the cosmetic and pharmaceutical industry, in particular as preservatives, exploring their other biological activities.


Asunto(s)
Cosméticos , Aceites Volátiles , Animales , Antibacterianos , Antifúngicos/farmacología , Cosméticos/farmacología , Aceites Volátiles/farmacología , Conservadores Farmacéuticos
6.
Colloids Surf B Biointerfaces ; 205: 111865, 2021 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-34044331

RESUMEN

Spreadability is one of the most important physicochemical properties of cosmetic products, according to the consumer. Thus, it is fundamental to develop strategies with the aim to improve the knowledge and predict the behavior of alternatives to synthetic emollients. The main goal of this research article was to correlate different physicochemical attributes, namely spreading value, apparent viscosity, density, saponification value, iodine value, peroxide value, acid value and melting range, with the spreading behavior of sustainable alternatives for petrolatum and dimethicone. The sensitivity and adequacy of each parameter were statistically analyzed, and the models were built by forward selection. The two adjusted and optimized models include viscosity and density as parameters and, in the petrolatum case, the model further includes the melting range, which was also validated as a significant predictor. Furthermore, it was also possible to compare the data obtained with the consumer's perception of the spreading behavior of the studied raw materials. A strong correlation was observed, suggesting that these tools mirror the consumer opinion. The application of these mathematical models is a valuable tool to assist the entire replacement process, which usually is a time-consuming procedure.


Asunto(s)
Cosméticos , Emolientes , Modelos Teóricos , Piel , Viscosidad
7.
Pharmaceutics ; 13(4)2021 Mar 30.
Artículo en Inglés | MEDLINE | ID: mdl-33808196

RESUMEN

The by-products of olive oil industry are a major ecological issue due to their phenolic content, highly toxic organic load, and low pH. However, they can be recovered and reused, since their components have antioxidant, anti-inflammatory, and photoprotector properties. In this work, oil-in-water creams containing three different olive oil industry by-products extracts were produced without the use of organic solvents. First, the extracts were thoroughly characterized in vitro for cytotoxicity, inhibition of skin enzymes, and antioxidant and photoprotection capacities. Safety studies were then performed, including ocular and skin irritation tests, ecotoxicity evaluation, and in vivo Human Repeat Insult Patch Test. The results obtained in this initial characterization supported the incorporation of the extracts in the cream formulations. After preparation, the creams were characterized for their organoleptic, physicochemical, droplet size and rheological properties, and microbial contamination. The results showed that all formulations were semi-solid creams, with stable pH, compatible with the skin, without microbial contamination, and with the expected droplet size range. The rheological analysis showed shear-thinning behavior with yield stress, with the viscosity decreasing with increasing shear rate. The oscillatory results suggest that the creams have a strong network structure, being easily rubbed into the skin. Finally, compatibility, acceptability and antioxidant efficacy were evaluated in vivo, in human volunteers. No adverse reactions were observed after application of the formulations on skin and the cream with the highest concentrations of phenolic compounds showed the highest antioxidant efficiency. In conclusion, the results suggest that olive oil industry by-products extracts have valuable properties that favor their re-use in the cosmetic industry. The example presented here showed their successful incorporation into creams and their impact in these formulations' appearance, pH, and rheological performance, as well as their in vivo compatibility with skin and antioxidant efficiency.

8.
Pharmaceutics ; 13(3)2021 Mar 03.
Artículo en Inglés | MEDLINE | ID: mdl-33802592

RESUMEN

Innovative formulations, including solid lipid nanoparticles (SLNs), have been sought to improve skin permeation of non-steroidal anti-inflammatory drugs (NSAIDs). The present study explores the use of SLNs, prepared using a fusion-emulsification method, to increase skin permeation and in vivo activity of two relevant NSAIDs: A liquid molecule (etofenamate) and a solid one (ibuprofen), formulated in a 2% hydroxypropyl methylcellulose gel through the gelation of SLN suspensions. Compritol® 888 ATO and Tween® 80 were used as a solid lipid and a surfactant, respectively. All production steps were up scalable, resulting in SLNs with high encapsulation efficiency (>90%), a mean particle size of <250 nm, a polydispersity index <0.2, and that were stable for 12 months. In vitro permeation, using human skin in Franz diffusion cells, showed increased permeation and similar cell viability in Df and HaCaT cell lines for SLN formulations when compared to commercial formulations of etofenamate (Reumon® Gel 5%) and ibuprofen (Ozonol® 5%). In vivo activity in the rat paw edema inflammation model showed that SLN hydrogels containing lower doses of etofenamate (8.3 times lower) and ibuprofen (16.6 times lower) produced similar effects compared to the commercial formulations, while decreasing edema and inflammatory cell infiltration, and causing no histological changes in the epidermis. These studies demonstrate that encapsulation in SLNs associated to a suitable hydrogel is a promising technological approach to NSAIDs dermal application.

9.
Molecules ; 25(21)2020 Oct 22.
Artículo en Inglés | MEDLINE | ID: mdl-33105792

RESUMEN

With the increasing debate on sustainability, there is a strong market trend to formulate more sustainable products for topical application. Several studies emphasize the potential applications of natural, organic, or green chemistry-derived ingredients, but comparative studies between conventional ingredients and sustainable alternatives are lacking. This type of study is considered an excellent baseline and time-saving strategy for future studies. In addition, one of the main challenges of replacing ingredients by sustainable alternatives in topical vehicles is to maintain high-quality products. Thus, the main goal of this research study was to create a well-defined strategy supported by specific experimental data for the development of sustainable topical vehicles with high-quality standards. The study was designed to evaluate the effects of replacing conventional ingredients (e.g., hydrocarbons, silicones, and preservatives) by sustainable ones on the physical, chemical, and microbiological features of topical emulsions. Additionally, in vivo assessment studies were performed to evaluate the safety, biological efficacy, and sensorial aspects of the developed formulations. The results obtained showed that the replacement of ingredients by sustainable alternatives has an effective impact on the physicochemical and structural properties of the emulsions, mainly on their rheological behavior. However, using appropriate strategies for ingredient selection and rheological adjustment, it is possible to overcome some barriers created by the use of natural raw materials, thus developing appealing and high-quality sustainable topical vehicles.


Asunto(s)
Portadores de Fármacos/química , Emulsiones/química , Excipientes/química , Administración Tópica , Dimetilpolisiloxanos/química , Portadores de Fármacos/administración & dosificación , Portadores de Fármacos/efectos adversos , Composición de Medicamentos , Emulsiones/administración & dosificación , Emulsiones/efectos adversos , Glicoles de Etileno/química , Vidrio/química , Humanos , Hidrocarburos/química , Aceites/química , Vaselina/química , Poliésteres/química , Tereftalatos Polietilenos/química , Reología , Siliconas/química , Ceras/química
10.
Antioxidants (Basel) ; 9(7)2020 Jul 11.
Artículo en Inglés | MEDLINE | ID: mdl-32664603

RESUMEN

Skin aging is a biological process influenced by intrinsic and extrinsic factors. The last ones, mainly exposure to UV radiation, increases reactive oxygen species (ROS) production leading to a loss of extracellular matrix, also enhanced by enzymatic degradation of matrix supporting molecules. Thus, and with the growing demand for eco-friendly skin products, natural compounds extracted from brown seaweeds revealed to be good candidates due to their broad range of bioactivities, especially as antioxidants. The aim of this study was to assess the dermo-cosmetic potential of different fractions obtained from the brown seaweed Fucus spiralis. For this purpose, in vitro antioxidant (Total Phenolic Content (TPC), 1,1-Diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity, Ferric Reducing Antioxidant Power (FRAP), Oxygen Radical Absorbance Capacity (ORAC)), anti-enzymatic (collagenase, elastase and hyaluronidase), antimicrobial, anti-inflammatory (NO production) and photoprotective (ROS production) capacities were evaluated. Although nearly all fractions evidenced antioxidant effects, fraction F10 demonstrated the highest antioxidant ability (EC50 of 38.5 µg/mL, DPPH assay), and exhibited a strong effect as an inhibitor of collagenase (0.037 µg/mL) and elastase (3.0 µg/mL). Moreover, this fraction was also the most potent on reducing ROS production promoted by H2O2 (IC50 of 41.3 µg/mL) and by UVB (IC50 of 31.3 µg/mL). These bioactivities can be attributed to its high content of phlorotannins, as evaluated by LC-MS analysis, reinforcing the potential of F. spiralis for further dermatological applications.

11.
Pharmaceutics ; 12(5)2020 Apr 26.
Artículo en Inglés | MEDLINE | ID: mdl-32357441

RESUMEN

Hypopigmentation is a progressive dermatological condition caused by a reduction in the skin pigment, melanin. Its treatment is considered a challenge due to the lack of a highly efficient single therapy. Currently, the main treatments include photochemotherapy, application of corticosteroids and immunosuppressants, and laser. Khellin-based gel-in-oil emulsions appear as a promising alternative since they ensure a concentration of the drug, a natural furanochromone, at the desired location, skin surface. Khellin promotes repigmentation as it forms a dark colored complex after solar irradiation. The aim of this study was the development and characterization (e.g., rheological behaviour, droplet size, tackiness, adhesion and spreadability) of three topical gel-in-oil emulsions prepared with different emollients, formulated through a cold emulsification process, and suitable for the incorporation of khellin. In vitro studies were performed to evaluate the drug release and permeation profiles across artificial membranes and excised human skin, respectively, using Franz-type vertical diffusion cells. The W/O emulsions developed showed macroscopic appearance, shear-thinning behavior with a mean droplet size from 3.28 to 4.28 µm, suitable for topical application. In vitro studies revealed permeation values of about 1% of khellin across the stratum corneum, making these gel-in-oil emulsions promising for preclinical and clinical studies. The cold process, being an easy and low energy production method, represents an innovative strategy to produce khellin-based gel-in-oil emulsions to treat patients with hypopigmentation.

12.
Pharmaceutics ; 12(4)2020 Apr 14.
Artículo en Inglés | MEDLINE | ID: mdl-32295247

RESUMEN

Human neutrophil elastase (HNE) is a serine protease that degrades matrix proteins. An excess of HNE may trigger several pathological conditions, such as psoriasis. In this work, we aimed to synthesize, characterize and formulate new HNE inhibitors with a 4-oxo-ß-lactam scaffold with less toxicity, as well as therapeutic index in a psoriasis context. HNE inhibitors with 4-oxo-ß-lactam scaffolds were synthesized and characterized by NMR, FTIR, melting point, mass spectrometry and elemental analysis. In vitro cytotoxicity and serine protease assays were performed. The compound with the highest cell viability (AAN-16) was selected to be incorporated in an emulsion (AAN-16 E) and in a microemulsion (AAN-16 ME). Formulations were characterized in terms of organoleptic properties, pH, rheology, droplet size distribution, in vitro drug release and in vivo psoriatic activity. All compounds were successfully synthesized according to analytical methodology, with good yields. Both formulations presented suitable physicochemical properties. AAN-16 E presented the most promising therapeutic effects in a murine model of psoriasis. Overall, new HNE inhibitors were synthesized with high and selective activity and incorporated into topical emulsions with potential to treat psoriasis.

13.
Antioxidants (Basel) ; 9(2)2020 Feb 14.
Artículo en Inglés | MEDLINE | ID: mdl-32074975

RESUMEN

Fragaria vesca L. (F. vesca), popularly known as wild strawberry, is a plant from the Rosaceae family, found in temperate and subtropical areas of the northern hemisphere. F. vesca leaves have been shown to have antiseptic, emollient, and dermatological protection properties, due to the presence of bioactive compounds, such as flavonoids, phenolic acids, ellagitannins, and proanthocyanidins. In this study, a F. vesca extract was obtained by an optimized extraction process, and was characterized by HPLC, ROS scavenging activity, cytotoxicity assays in HaCaT cells, and tyrosinase inhibitory activity determination. The most active extract was then incorporated in a hydrogel with hydroxyethylcellulose at 2% (w/w), which was characterized at the physicochemical, stability, cytotoxicity, and ROS scavenging activity levels to evaluate its quality, safety, and efficacy. In vivo studies, human repeat insult patch testing, and an assay to determine their antioxidant efficacy, were also performed. The results showed that the Fragaria vesca extracts had antioxidant activity and that the F. vesca extract-based hydrogel exhibited cutaneous compatibility, acceptability and antioxidant efficacy, being stable, and suitable for topical application.

14.
Mol Neurobiol ; 57(5): 2391-2419, 2020 May.
Artículo en Inglés | MEDLINE | ID: mdl-32062841

RESUMEN

Psoriasis is a chronic immune-mediated skin disease, with a pathogenesis resulting from a combination of genetic and environmental factors. The pathogenesis of psoriasis is driven by the interaction between innate and adaptive immune cells and keratinocytes, in a complex process mediated by cytokines and other signaling molecules. This leads to an inflammatory process with increased proliferation of epidermal cells, neo-angiogenesis, and infiltration of white cells in the skin, which cause the characteristic psoriasis plaques. Several studies have suggested that the neurotransmitter serotonin, a key mediator between the skin and the neuroendocrine system, also plays an important role in the pathogenesis of psoriasis. Psoriasis often needs long-term treatment, which can be a burden. Thus, the choice of the treatment is crucial to increase the patients' adherence and quality of life. This review addresses the currently available systemic and topical treatments for psoriasis, used by themselves or combined with phototherapy. It particularly focuses on the importance of advanced drug delivery systems as a way to increase the drug penetration and retention in the skin, while also enhancing its solubility and stability. Finally, we discuss the role of the serotonin system in psoriasis, and summarize what is known about the effects of antidepressants, in particular specific serotonin reuptake inhibitors, on the physical symptoms of this disease.


Asunto(s)
Fármacos Dermatológicos/uso terapéutico , Psoriasis/tratamiento farmacológico , Serotoninérgicos/uso terapéutico , Serotonina/fisiología , Administración Oral , Administración Tópica , Antiinflamatorios/administración & dosificación , Antiinflamatorios/uso terapéutico , Antidepresivos/administración & dosificación , Antidepresivos/uso terapéutico , Productos Biológicos/administración & dosificación , Productos Biológicos/uso terapéutico , Biosimilares Farmacéuticos/administración & dosificación , Biosimilares Farmacéuticos/uso terapéutico , Ensayos Clínicos como Asunto , Fármacos Dermatológicos/administración & dosificación , Formas de Dosificación , Sistemas de Liberación de Medicamentos , Emulsiones , Predicción , Terapia Genética , Humanos , Factores Inmunológicos/administración & dosificación , Factores Inmunológicos/uso terapéutico , Inmunosupresores/administración & dosificación , Inmunosupresores/uso terapéutico , Liposomas , Terapia por Luz de Baja Intensidad , Nanopartículas , Fototerapia , Psoriasis/metabolismo , Psoriasis/radioterapia , Psoriasis/terapia , Serotoninérgicos/administración & dosificación , Inhibidores Selectivos de la Recaptación de Serotonina/administración & dosificación , Inhibidores Selectivos de la Recaptación de Serotonina/uso terapéutico
15.
Antioxidants (Basel) ; 8(10)2019 Oct 01.
Artículo en Inglés | MEDLINE | ID: mdl-31581509

RESUMEN

The aim of this study was to develop a phytocosmetic sunscreen emulsion with antioxidant effect, containing a blend of flavonoid-enriched plant extracts. In vitro sun protection factor, antioxidant activity, skin irritation, photostability, cutaneous permeation, and retention of flavonoids were evaluated. Thermodynamically stable emulsions were obtained and tested for sensorial analysis after loading the blend of extracts. The selected emulsion was stable when stored at low temperatures (5 C), for which after 120 days the concentration of quercetin and rutin were above their limit of quantification, i.e., 2.8 ± 0.39 µg/mL and 30.39 ± 0.39 µg/mL, respectively. Spreadability, low rupture strength and adhesiveness were shown to be similar to a conventional topical product. Higher brittleness, pseudo-plastic, and viscoelastic behaviors were also recorded for the developed phytocosmetic sunscreen. The product presented a critical wavelength of 387.0 nm and ultraviolet rays A and B (UVA/UVB) rate of 0.78, confirming that the developed formulation shows capacity for UVA/UVB protection, protecting skin against damages caused by Ultraviolet (UV) radiation. Rutin was shown to permeate the skin barrier and was also quantified in the stratum corneum (3.27 ± 1.92 µg/mL) by tape stripping and retention test (114.68 ± 8.70 µg/mL). The developed flavonoid-enriched phytocosmetic was shown to be non-irritant to skin by an in vitro assay. Our results confirm the antioxidant activity, sun protection, and physical properties of the developed phytocosmetic for topical application.

16.
Polymers (Basel) ; 11(1)2019 Jan 10.
Artículo en Inglés | MEDLINE | ID: mdl-30960092

RESUMEN

The present study investigated a new approach to treat superficial skin infections by topical application of minocycline hydrochloride (MH) formulated in a novel starch-based Pickering emulsion (ASt-emulsions). The emulsions were fully characterized in terms of efficacy, as well as in vitro release and permeation studies. The emulsions provided a prolonged MH release, always above its minimum inhibitory concentration against Staphylococcus aureus, although the drug did not permeate through the entire skin layer. The in vitro antibacterial activity of MHASt-emulsions against S. aureus was confirmed and their therapeutic efficacy was assessed using an in vitro skin-adapted agar diffusion test. In vivo antibacterial activity, evaluated using the tape-stripping infection model in mice, showed the topical administration of MH was effective against superficial infections caused by S. aureus. This study supports the potential of ASt-emulsions as promising platforms for topical antibiotic delivery, contributing to a new perspective on the treatment of superficial bacterial infections.

17.
Pharmaceutics ; 11(3)2019 Mar 19.
Artículo en Inglés | MEDLINE | ID: mdl-30893873

RESUMEN

Quercus Suber Bark from Quercus suber L. is a natural, renewable and biodegradable biomaterial with multifunctional proprieties. In this study, we used it as solid particles to stabilize a Pickering emulsion. The main goal was to produce an optimized topical formulation using biocompatible organic particles as stabilizers of the emulsion instead of the common surfactants, whilst benefiting from Quercus suber L. proprieties. In this work, a Quality by Design (QbD) approach was successfully applied to the production of this emulsion. A screening design was conducted, identifying the critical variables of the formula and process, affecting the critical quality attributes of the emulsion (droplet size distribution). The optimization of the production was made through the establishment of the design space. The stability was also investigated during 30 days, demonstrating that Quercus Suber Bark-stabilized emulsions are stable since the droplet size distribution lowers. In vitro studies were performed to assess antioxidant and antiaging efficacy, which revealed that the formulation had indeed antioxidant proprieties. A physicochemical characterization demonstrated that the formulation presents a shear-thinning fluid, ideal for topical administration. The in vivo compatibility study confirmed that the final formulation is not skin irritant, being safe for human use. A sensorial analysis was also performed, using a simple sensory questionnaire, revealing very positive results. Thus, the use of Quercus Suber Bark particles as a multifunctional solid ingredient contributed to achieve a stable, effective and innovative Pickering emulsion with a meaningful synergistic protection against oxidative stress.

18.
AAPS PharmSciTech ; 20(1): 9, 2018 Dec 17.
Artículo en Inglés | MEDLINE | ID: mdl-30560393

RESUMEN

The aim of study was to determine the in vitro sun protection factor (SPF) and the photostability profile of a topical formulation composed of nanoparticles loaded with vegetable extracts and to assess its physicochemical properties. Chitosan/tripolyphosphate (TPP) nanoparticles loaded with flavonoids-enriched vegetable extracts (Ginkgo biloba L., Dimorphandra mollis Benth, Ruta graveolens, and Vitis vinifera L.) were produced and characterized for their morphology, mean particle size, zeta potential, and encapsulation efficiency. A final topical formulation was obtained by dispersing chitosan/TPP nanoparticles in an o/w emulsion. Results showed that nanoparticles dispersion exhibited yellowish color, spherical shape, and uniform appearance. Extract-loaded chitosan/TPP nanoparticles showed a mean particle size of 557.11 ± 3.1 nm, polydispersity index of 0.39 ± 0.27, zeta potential of + 11.54 ± 2.1 mV, and encapsulation efficiency of 75.89% of rutin. The recorded texture parameters confirm that the developed formulation is appropriate for skin application. The SPF obtained was 2.3 ± 0.4, with a critical wavelength of 387.0 nm and 0.69 UVA/UVB ratio. The developed formulation exhibited photostability, allowing the release of flavonoids from nanoparticles while retaining rutin into the skin in a higher extension.


Asunto(s)
Flavonoides/química , Extractos Vegetales/química , Factor de Protección Solar , Quitosano/análogos & derivados , Quitosano/química , Estabilidad de Medicamentos , Emulsiones/química , Ginkgo biloba , Nanopartículas/química , Tamaño de la Partícula , Extractos Vegetales/análisis
19.
Pharmaceutics ; 10(4)2018 Dec 13.
Artículo en Inglés | MEDLINE | ID: mdl-30551686

RESUMEN

Onychomycosis affects about 15% of the population. This disease causes physical and psychosocial discomfort to infected patients. Topical treatment (creams, solutions, gels, colloidal carriers, and nail lacquers) is usually the most commonly required due to the high toxicity of oral drugs. Currently, the most common topical formulations (creams and lotions) present a low drug delivery to the nail infection. Nail lacquers appear to increase drug delivery and simultaneously improve the effectiveness of treatment with increased patient compliance. These formulations leave a polymer film on the nail plate after solvent evaporation. The duration of the film residence in the nail constitutes an important property of nail lacquer formulation. In this study, a polyurethane polymer was used to delivery antifungals drugs, such as terbinafine hydrochloride (TH) and ciclopirox olamine (CPX) and the influence of its concentration on the properties of nail lacquer formulations was assessed. The nail lacquer containing the lowest polymer concentration (10%) was the most effective regarding the in vitro release, permeation, and antifungal activity. It has also been demonstrated that the application of PU-based nail lacquer improves the nail plate, making it smooth and uniform and reduces the porosity contributing to the greater effectiveness of these vehicles. To conclude, the use of polyurethane in nail formulations is promising for nail therapeutics.

20.
Pharmaceutics ; 10(3)2018 Aug 01.
Artículo en Inglés | MEDLINE | ID: mdl-30071584

RESUMEN

Polymer-based eye drops are the most used drug delivery system to treat dry eye disease (DED). Therefore, the mucoadhesion between the polymer and the ocular mucin is crucial to ensure the efficacy of the treatment. In this context, the present study aimed to evaluate the potential use of in vitro methods to study the mucoadhesion of eye drop solutions and, specifically to evaluate the efficacy of two hyaluronic acid-based formulations (HA), HA 0.15% and 0.30% (w/v) to treat DED. Rheology methods and zeta potential determination were used to study the mucoadhesive properties of both eye drop solutions. All results indicated that interactions occurred between the mucin and the HA, being stronger with HA 0.30%, due to the physical entanglements and hydrogen bounding. In vitro tests on ARPE-19 cell line were performed using a 2D and a 3D dry eye model and the results have shown that pre-treated cells with HA showed a morphology more similar to the hydrated cells in both products, with a high survival rate. The in vitro techniques used in this study have been shown to be suitable to evaluate and predict mucoadhesive properties and the efficacy of the eye drops on relief or treatment of DED. The results obtained from these methods may help in inferring possible in vivo effects.

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