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Manna, a very singular vegetable product derived from the spontaneous solidification of the sap of some Fraxinus species, has long been known for its mild laxative and emollient properties. In this work, a hydro-alcoholic extract of manna (HME) from Sicilian Fraxinus angustifolia Vahl was investigated using HPLC-DAD to find phenol components and using chemical and biological in vitro assays to determine its reducing, antioxidant and anti-inflammatory capacity. We identified elenolic acid, tyrosol, hydroxytyrosol, catechin, fraxetin, verbascoside, gallic acid, procyanidin-B1, and luteolin 3,7 glucoside, in order of abundance. Measurements of total antioxidant activity by Folin-Ciocalteu reaction and ferric reducing ability (FRAP), as well as of scavenger activity towards ABTSâ¢+, DPPHâ¢, and perferryl-myoglobin radicals, showed that the phytocomplex effectively reduced oxidants with different standard potentials. When compared with vitamin E, HME also behaved as an efficient chain-breaking antioxidant against lipoperoxyl radicals from methyl linoleate. In cellular models for oxidative stress, HME counteracted membrane lipid oxidation of human erythrocytes stimulated by tert-butyl hydroperoxide and prevented the generation of reactive oxygen species, as well as the GSH decay in IL-1ß-activated intestinal normal-like cells. Moreover, in this in vitro intestinal bowel disease model, HME reduced the release of the pro-inflammatory cytokines IL-6 and IL-8. These findings may suggest that manna acts as an antioxidant and anti-inflammatory natural product in humans, beyond its well-known effects against constipation.
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In this work the HPLC and NMR analysis of the phenyl-ethanoid glycosides (PhGs) pattern of a cultivated exemplar of Verbascum thapsus L. (Scrophulariaceae) from the Etnean area (Sicily, Italy) was performed in order to verify their possible presence. Wild V. thapsus is well-known in ethnopharmacology due to the several beneficial effects that it is able to exert and which are primarily due to these compounds. So, it's extremely important that also cultivated exemplars of this species biosynthesize them in order to maintain their pharmacological properties. This study revealed the presence of seven PhGs in an unusual novel pattern. Thus, this exemplar is a very good potential source of this class of natural products and may be employed for several beneficial ethnopharmacological purposes.
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Cromatografía Líquida de Alta Presión/métodos , Glicósidos/análisis , Glicósidos/química , Espectroscopía de Resonancia Magnética/métodos , Verbascum/química , Estructura Molecular , Extractos Vegetales/análisis , Extractos Vegetales/química , Plantas Medicinales/química , Sicilia , Espectrometría de Masas en Tándem , Verbascum/crecimiento & desarrolloRESUMEN
Skin aging is a complex biological process influenced by a combination of endogenous or intrinsic and exogenous or extrinsic factors due to environmental damage. The primary environmental factor that causes human skin aging is the ultraviolet irradiation from the sun. Recently, it was established that the long-term exposure to light-emitting-diode-generated blue light (LED-BL) from electronic devices seems to have a relevant implication in the molecular mechanisms of premature photoaging. BL irradiation induces changes in the synthesis of various skin structures through DNA damage and overproduction of reactive oxygen species (ROS), matrix metalloproteinase-1 and -12, which are responsible for the loss of the main components of the extracellular matrix of skin like collagen type I and elastin. In the current study, using human keratinocytes and fibroblasts exposed to specific LED-BL radiation doses (45 and 15 J/cm 2 ), we produced an in vitro model of skin photoaging. We verified that, compared with untreated controls, the treatment with LED-BL irradiation results in the alteration of metalloprotease-1 (collagenase), metalloprotease-12 (elastase), 8-dihydroxy-2'-deoxyguanosine, proliferating cell nuclear antigen, and collagen type I. Moreover, we showed that the photoaging prevention is possible via the use of hydroxytyrosol extracted from olive fruits, well known for antioxidant properties. Our results demonstrated that hydroxytyrosol protects keratinocytes and fibroblasts from LED-BL-induced damage. Thus, hydroxytyrosol might be proposed as an encouraging candidate for the prevention of BL-induced premature photoaging.
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Antioxidantes/farmacología , Fibroblastos/efectos de los fármacos , Frutas , Queratinocitos/efectos de los fármacos , Luz/efectos adversos , Olea , Alcohol Feniletílico/análogos & derivados , Protectores contra Radiación/farmacología , Envejecimiento de la Piel/efectos de los fármacos , Piel/efectos de los fármacos , Antioxidantes/aislamiento & purificación , Línea Celular , Supervivencia Celular/efectos de los fármacos , Supervivencia Celular/efectos de la radiación , Colágeno Tipo I/genética , Colágeno Tipo I/metabolismo , Daño del ADN , Elastina/metabolismo , Fibroblastos/metabolismo , Fibroblastos/patología , Fibroblastos/efectos de la radiación , Frutas/química , Humanos , Queratinocitos/metabolismo , Queratinocitos/patología , Queratinocitos/efectos de la radiación , Metaloproteinasa 1 de la Matriz/genética , Metaloproteinasa 1 de la Matriz/metabolismo , Metaloproteinasa 12 de la Matriz/genética , Metaloproteinasa 12 de la Matriz/metabolismo , Olea/química , Estrés Oxidativo/efectos de los fármacos , Estrés Oxidativo/efectos de la radiación , Alcohol Feniletílico/aislamiento & purificación , Alcohol Feniletílico/farmacología , Antígeno Nuclear de Célula en Proliferación/metabolismo , Protectores contra Radiación/aislamiento & purificación , Especies Reactivas de Oxígeno/metabolismo , Piel/metabolismo , Piel/patología , Piel/efectos de la radiación , Envejecimiento de la Piel/efectos de la radiación , Factores de TiempoRESUMEN
Obesity and metabolic disorders can be risk factors for the onset and development of neurodegenerative diseases. The aim of the present study was to investigate the protective effects of a natural dietary supplement (NDS), containing Curcuma longa, silymarin, guggul, chlorogenic acid and inulin, on dysmetabolism and neurodegeneration in the brains of high fat diet (HFD)-fed mice. Decrease in the expression of FACL-4, CerS-1, CerS-4, cholesterol concentration and increase in the insulin receptor expression and insulin signaling activation, were found in brains of NDS-treated HFD brains in comparison with HFD untreated-mice, suggesting that NDS is able to prevent brain lipid accumulation and central insulin resistance. In the brains of NDS-treated HFD mice, the levels of RNS, ROS and lipid peroxidation, the expression of p-ERK, H-Oxy, i-NOS, HSP60, NF-kB, GFAP, IL-1ß, IL-6 and CD4 positive cell infiltration were lower than in untreated HFD mice, suggesting antioxidant and anti-inflammatory effects of NDS. The decreased expression of p-ERK and GFAP in NDS-treated HFD mice was confirmed by immunofluorescence. Lastly, a lower number of apoptotic nuclei was found in cortical sections of NDS-treated HFD mice. The present data indicate that NDS exerts neuroprotective effects in HFD mice by reducing brain fat accumulation, oxidative stress and inflammation and improving brain insulin resistance.
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Antiinflamatorios/farmacología , Antioxidantes/farmacología , Encéfalo/efectos de los fármacos , Dieta Alta en Grasa , Suplementos Dietéticos , Degeneración Nerviosa , Enfermedades Neurodegenerativas/prevención & control , Animales , Apoptosis/efectos de los fármacos , Encéfalo/metabolismo , Encéfalo/patología , Modelos Animales de Enfermedad , Mediadores de Inflamación/metabolismo , Insulina/metabolismo , Resistencia a la Insulina , Metabolismo de los Lípidos/efectos de los fármacos , Peroxidación de Lípido/efectos de los fármacos , Masculino , Ratones Endogámicos C57BL , Enfermedades Neurodegenerativas/metabolismo , Enfermedades Neurodegenerativas/patología , Estrés Oxidativo/efectos de los fármacos , Transducción de Señal/efectos de los fármacosRESUMEN
Introduction: Gradual population aging is creating a new set of needs in the general population. Memory capacity decreases with age, and memory deficits are considered an early symptom of Alzheimer's Disease (AD), one of the most prevalent cognitive disorders in older people. Numerous studies have shown that grape polyphenolic compounds (GPs) are able to attenuate cognitive impairment and reduce brain lesions in experimental AD animal models. These GP effects are associated with improvement in brain antioxidant status and prevention of free radical-induced neuronal damage. We designed a randomized, double-blind, placebo-controlled clinical trial to investigate the potential beneficial effects of a Vitis vinifera-based dietary supplement on cognitive function and neuropsychological status in healthy older adults. Methods: One-hundred eleven subjects were recruited and randomly divided in two groups: one group received the V. vinifera-based dietary supplement Cognigrape® for 12 weeks (250 mg/day) and the second group received placebo over the same period of time. Before and after the end of the supplementation period, cognitive function and neuropsychological status were evaluated using the Mini-Mental State Examination (MMSE), Beck Depression Inventory (BDI), Hamilton Anxiety Rating Scale (HARS), and Repeatable Battery for the Assessment of Neuropsychological Status (RBANS) evaluations. Results: MMSE scores were significantly improved after supplementation with Cognigrape® in comparison with baseline levels (p < 0.0001) and placebo (r = 0.59, 0.95% CI 0.11, 1.22; p < 0.0001). Cognigrape® supplementation produced a significant reduction in BDI (-15.8%) and HARS (-24.9%) scores with respect to baseline levels (p < 0.0001) and placebo (p < 0.0001 for BDI and p < 0.05 for HARS). RBANS total score was significantly improved by Cognigrape® with respect to baseline levels and placebo (r = 0.55, 0.95% CI 0.48, 6.07; p < 0.0001). The comparison with the placebo revealed improvements in several parameters among participants receiving Cognigrape®: attention (p < 0.001); language (p < 0.05); immediate memory (p < 0.0001); and delayed memory (p < 0.0001). Visuospatial/constructional abilities were not modified. During the study, no adverse effects were detected. Conclusion: The results show that 12 weeks of Cognigrape® supplementation is safe, can improve physiological cognitive profiles, and can concurrently ameliorate negative neuropsychological status in healthy older adults.
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Metalloproteases are a family of zinc-containing endopeptidases involved in a variety of pathological disorders. The use of flavonoid derivatives as potential metalloprotease inhibitors has recently increased.Particular plants growing in Sicily are an excellent yielder of the flavonoids luteolin, apigenin, and their respective glycoside derivatives (7-O-rutinoside, 7-O-glucoside, and 7-O-glucuronide).The inhibitory activity of luteolin, apigenin, and their respective glycoside derivatives on the metalloproteases MMP-1, MMP-3, MMP-13, MMP-8, and MMP-9 was assessed and rationalized correlating in vitro target-oriented screening and in silico docking.The flavones apigenin, luteolin, and their respective glucosides have good ability to interact with metalloproteases and can also be lead compounds for further development. Glycones are more active on MMP-1, -3, -8, and -13 than MMP-9. Collagenases MMP-1, MMP-8, and MMP-13 are inhibited by compounds having rutinoside glycones. Apigenin and luteolin are inactive on MMP-1, -3, and -8, which can be interpreted as a better selectivity for both -9 and -13 peptidases. The more active compounds are apigenin-7-O-rutinoside on MMP-1 and luteolin-7-O-rutinoside on MMP-3. The lowest IC50 values were also found for apigenin-7-O-glucuronide, apigenin-7-O-rutinoside, and luteolin-7-O-glucuronide. The glycoside moiety might allow for a better anchoring to the active site of MMP-1, -3, -8, -9, and -13. Overall, the in silico data are substantially in agreement with the in vitro ones (fluorimetric assay).
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Flavonoides/farmacología , Inhibidores de la Metaloproteinasa de la Matriz/farmacología , Apigenina/química , Apigenina/farmacología , Sistemas de Liberación de Medicamentos , Luteolina/química , Luteolina/farmacología , Inhibidores de la Metaloproteinasa de la Matriz/química , Inhibidores de la Metaloproteinasa de la Matriz/aislamiento & purificación , Metaloproteinasas de la Matriz , Simulación del Acoplamiento MolecularRESUMEN
Sesamol is a natural phenolic compound extracted from Sesamum indicum seed oil. Sesamol is endowed with several beneficial effects, but its use as a topical agent is strongly compromised by unfavorable chemical-physical properties. Therefore, to improve its characteristics, the aim of the present work was the formulation of nanostructured lipid carriers as drug delivery systems for topical administration of sesamol.Two different nanostructured lipid carrier systems have been produced based on the same solid lipid (Compritol® 888 ATO) but in a mixture with two different kinds of oil phase such as Miglyol® 812 (nanostructured lipid carrier-M) and sesame oil (nanostructured lipid carrier-PLUS). Morphology and dimensional distribution of nanostructured lipid carriers have been characterized by differential scanning calorimetry and photon correlation spectroscopy, respectively. The release pattern of sesamol from nanostructured lipid carriers was evaluated in vitro determining drug percutaneous absorption through excised human skin. Furthermore, an oxygen radical absorbance capacity assay was used to determine their antioxidant activity.From the results obtained, the method used to formulate nanostructured lipid carriers led to a homogeneous dispersion of particles in a nanometric range. Sesamol has been encapsulated efficiently in both nanostructured lipid carriers, with higher encapsulation efficiency values (> 90â%) when sesame oil was used as the oil phase (nanostructured lipid carrier-PLUS). In vitro evidences show that nanostructured lipid carrier dispersions were able to control the rate of sesamol diffusion through the skin, with respect to the reference formulations.Furthermore, the oxygen radical absorbance capacity assay pointed out an interesting and prolonged antioxidant activity of sesamol, especially when vehiculated by nanostructured lipid carrier-PLUS.
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Antioxidantes/administración & dosificación , Benzodioxoles/administración & dosificación , Nanoestructuras , Vehículos Farmacéuticos , Fenoles/administración & dosificación , Administración Tópica , Adulto , Antioxidantes/farmacología , Benzodioxoles/química , Benzodioxoles/farmacología , Humanos , Técnicas In Vitro , Lípidos , Estructura Molecular , Tamaño de la Partícula , Fenoles/química , Fenoles/farmacología , Absorción CutáneaRESUMEN
INTRODUCTION: Colloidal drug delivery systems (CDDSs) are innovative carriers that have been studied in pharmaceutical field from many years to overcome unfavorable physical and chemical features of synthetic drugs. Recently the use of CDDS as carriers for phytochemicals has seen an exponential increase which, in some cases, has led to the rediscovery of ancient and forgotten natural molecules. Area covered: This article focuses on the main features of CDDS, particularly micro- and nanoemulsions, vesicular carriers and micro- and nanoparticles, loaded with natural active compounds. A detailed review of the literature is presented, introducing the importance of these systems in terms of their capability to optimize the stability of phytochemicals, their absorption through biological membranes and their bioavailability. Expert opinion: The delivery of phytochemicals is problematic due to poor solubility, poor permeability, low bioavailability, instability in biological milieu and extensive first-pass metabolism. Global research efforts investigating nanotechnology have attempted to overcome these limitations rediscovering and, in some cases, 'discovering ex novo' unexpected virtues and benefits associated to these compounds. The 'nanotechnological approach' can definitely enhance the pharmacokinetics and therapeutic index of natural active compounds and improve their performance in therapy.
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Productos Biológicos/administración & dosificación , Sistemas de Liberación de Medicamentos , Nanotecnología , Disponibilidad Biológica , Portadores de Fármacos/química , Humanos , Nanopartículas , Preparaciones Farmacéuticas/administración & dosificación , SolubilidadRESUMEN
The Opuntia ficus-indica multiple properties are reflected in the increasing interest of chemists in the identification of its natural components having pharmaceutical and/or cosmetical applications. Here we report the structural elucidation of Opuntia ficus-indica mucilage that highlighted the presence of components differing for their chemical nature and the molecular weight distribution. The high molecular weight components were identified as a linear galactan polymer and a highly branched xyloarabinan. The low molecular weight components were identified as lactic acid, D-mannitol, piscidic, eucomic and 2-hydroxy-4-(4'-hydroxyphenyl)-butanoic acids. A wound healing assay was performed in order to test the cicatrizing properties of the various components, highlighting the ability of these latter to fasten dermal regeneration using a simplified in vitro cellular model based on a scratched keratinocytes monolayer. The results showed that the whole Opuntia mucilage and the low molecular weight components are active in the wound repair.
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Queratinocitos/efectos de los fármacos , Opuntia/química , Polisacáridos/química , Cicatrización de Heridas/efectos de los fármacos , Humanos , Peso MolecularRESUMEN
Gastroesophageal reflux (GER) is a common, chronic, relapsing symptom. Often people self-diagnose and self-treat it even though health-related quality of life is significantly impaired. In the lack of a valid alternative approach, current treatments focus on suppression of gastric acid secretion by the use of proton pump inhibitors (PPIs), but people with GER have a significantly lower response rate to therapy. We designed a randomized double-blinded controlled clinical study to evaluate the efficacy and the safety of a formulation based on sodium alginate/bicarbonate in combination with extracts obtained from Opuntia ficus-indica and Olea europaea associated with polyphenols (Mucosave®; verum), on GER-related symptoms. Male/female 118 (intention to treat) subjects with moderate GER and having at least 2 to 6 days of GER episodes/week were treated with verum (6 g/day) or placebo for two months. The questionnaires Gastroesophageal Reflux Disease-Health-Related Quality of Life (GERD-HRQoL) and Gastroesophageal Reflux Disease Symptom Assessment Scale (GSAS) were self-administered by participants before the treatment and at the end of the treatment. Verum produced statistically significant reduction of GERD-HRQoL and GSAS scores, -56.5% and -59.1%, respectively, in comparison to placebo. Heartburn and acid regurgitation episodes for week were significantly reduced by verum (p < 0.01). Results indicate that Mucosave formulation provides an effective and well-tolerated treatment for reducing the frequency and intensity of symptoms associated with gastroesophageal reflux.
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The aim of this research was to assess the impact of a well-characterized extract from Citrus bergamia juice on adipogenesis and/or lipolysis using mesenchymal stem cells from human adipose tissue as a cell model. To evaluate the effects on adipogenesis, some cell cultures were treated with adipogenic medium plus 10 or 100 µg/mL of extract. To determine the properties on lipolysis, additional mesenchymal stem cells were cultured with adipogenic medium for 14 days and after this time added with Citrus bergamia for further 14 days. To verify adipogenic differentiation, oil red O staining at 7, 14, 21, and 28 days was performed. Moreover, the expression of peroxisome proliferator-activated receptor gamma (PPAR-γ), adipocytes fatty acid-binding protein (A-FABP), adipose triglyceride lipase (ATGL), hormone-sensitive lipase (HSL), monoglyceride lipase (MGL), 5'-adenosine monophosphate-activated protein kinase (AMPK)α1/2, and pAMPKα1/2 was evaluated by Western blot analysis and the release of glycerol by colorimetric assay. Citrus bergamia extract suppressed the accumulation of intracellular lipids in mesenchymal stem cells during adipogenic differentiation and promoted lipolysis by repressing the expression of adipogenic genes and activating lipolytic genes. Citrus bergamia extract could be a useful natural product for improving adipose mobilization in obesity-related disorders.
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In this study, we evaluated different strategies to optimize the percutaneous absorption of niacinamide (NA) and soy phytosterols (FITO) by making use of solid lipid nanoparticles (SLN) and penetration enhancers, such as the hydrogenated lecithin. The evaluation of the skin permeation of NA and FITO has been effected in vitro using excised human skin (i.e., stratum corneum-epidermis or SCE). Furthermore, we evaluated the in vivo effect that NA and FITO has on skin barrier recovery after the topical application; using the extent of methyl nicotinate (MN)-induced erythema in damaged skin as a parameter to determine the rate of stratum corneum recovery. Results pointed out the importance of these strategies as valid tools for NA and FITO topical delivery. In fact, soy lecithin based formulations were able to increase the percutaneous absorption of the two active ingredients, while SLN guaranteed an interesting delayed and sustained release of FITO. In vivo evaluation showed clearly that the formulation containing both the actives (NA and FITO) is able to recover about 95% of skin barrier integrity eight days after tape stripping. This effect is probably due to the "synergistic effect" of NA and FITO.
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Niacinamida/química , Niacinamida/metabolismo , Fitosteroles/química , Fitosteroles/metabolismo , Absorción Cutánea , Piel/metabolismo , Administración Tópica , Adulto , Química Farmacéutica/métodos , Portadores de Fármacos/química , Epidermis/metabolismo , Femenino , Humanos , Lecitinas/química , Lípidos/química , Masculino , Nanopartículas/química , Ácidos Nicotínicos/química , PermeabilidadRESUMEN
CONTEXT: Solid lipid nanoparticles (SLN) are drug carriers possessing numerous features useful for topical application. A copious scientific literature outlined their ability as potential delivery systems for lipophilic drugs, while the entrapment of a hydrophilic drug inside the hydrophobic matrix of SLN is often difficult to obtain. OBJECTIVE: To develop SLN intended for loading caffeine (SLN-CAF) and to evaluate the permeation profile of this substance through the skin once released from the lipid nanocarriers. Caffeine is an interesting compound showing anticancer and protective effects upon topical administration, although its penetration through the skin is compromised by its hydrophilicity. MATERIALS AND METHODS: SLN-CAF were formulated by using a modification of the quasi-emulsion solvent diffusion technique (QESD) and characterized by PCS and DSC analyses. In vitro percutaneous absorption studies were effected using excised human skin membranes (i.e. Stratum Corneum Epidermis or SCE). RESULTS: SLN-CAF were in a nanometric range (182.6 ± 8.4 nm) and showed an interesting payload value (75% ± 1.1). DSC studies suggest the presence of a well-defined system and the successful drug incorporation. Furthermore, SLN-CAF generated a significantly faster permeation than a control formulation over 24 h of monitoring. DISCUSSION AND CONCLUSIONS: SLN-CAF were characterized by valid dimensions and a good encapsulation efficiency, although the active to incorporate showed a hydrophilic character. This result confirms the suitability of the formulation strategy employed in the present work. Furthermore, the in vitro evidence outline the key role of lipid nanoparticles in enhancing caffeine permeation through the skin.
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Cafeína/administración & dosificación , Cafeína/farmacocinética , Estimulantes del Sistema Nervioso Central/administración & dosificación , Estimulantes del Sistema Nervioso Central/farmacocinética , Lípidos/química , Nanopartículas/química , Administración Tópica , Adulto , Algoritmos , Cafeína/química , Estimulantes del Sistema Nervioso Central/química , Portadores de Fármacos , Sistemas de Liberación de Medicamentos , Diseño de Fármacos , Humanos , Técnicas In Vitro , Tamaño de la Partícula , Absorción CutáneaRESUMEN
Ophthalmic diseases collect great attention by researchers and pharmaceutical technologists, since they can dramatically worsen the quality of life. Because of the limited duration of action on the eye surface, and anatomical/physiological barriers to drug penetration from it into the inner eye structures, conventional ocular formulations are generally unable to perform at their best. Nanotechnology approaches can represent a solution to improve the therapeutic efficiency, compliance and safety of ocular drugs. In this respect, lipid-based nanocarriers are among the most interesting systems. Their composition and production methods make them highly biocompatible and safe formulations. This review illustrates the developments achieved in ocular drug delivery using lipid-based nanocarriers, with a critical revision of recent scientific articles and filed patents.
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Portadores de Fármacos/administración & dosificación , Lípidos/administración & dosificación , Nanopartículas/administración & dosificación , Patentes como Asunto , Administración Oftálmica , Portadores de Fármacos/química , Oftalmopatías , Humanos , Lípidos/química , Nanopartículas/químicaRESUMEN
The peculiar physio-anatomical structure of the eye and the poor physico-chemical properties of many drug molecules are often responsible for the inefficient treatment of ocular diseases by conventional dosage forms, and justify the development of innovative ocular drug delivery systems. Lipid-based nanocarriers (LNC) are among the newer and interesting colloidal drug delivery systems; they show the capability to improve the local bioavailability of drugs administered by various ocular routes and, therefore, their therapeutic efficacy. Furthermore, their extreme biodegradability and biocompatible chemical nature have secured them the title of 'nanosafe carriers.' This review treats the main features of LNC [namely, solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC) and lipid-drug conjugates (LDC)]; examples and advantages of the application of these colloidal carrier systems for the ophthalmic administration of drugs are presented.
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Portadores de Fármacos/química , Ojo/metabolismo , Lípidos/química , Nanomedicina/métodos , Nanoestructuras , Animales , Oftalmopatías/tratamiento farmacológico , Oftalmopatías/genética , HumanosRESUMEN
The increased awareness of protection against UV radiation damages has led to a rise in the use of topically applied chemical sunscreen agents and to an increased need of innovative carriers designed to achieve the highest protective effect and reduce the toxicological risk resulting from the percutaneous absorption of these substances. In this paper, nanostructured lipid carriers (NLC) and nanoemulsions (NE) were formulated to optimize the topical application of different and widespread UVA or UVB sun filters (ethyl hexyltriazone (EHT), diethylamino hydroxybenzoyl hexyl benzoate (DHHB), bemotrizinol (Tinosorb S), octylmethoxycinnamate (OMC) and avobenzone (AVO)). The preparation and stability parameters of these nanocarriers have been investigated concerning particle size and zeta potential. The release pattern of the sunscreens from NLC and NE was evaluated in vitro, determining their percutaneous absorption through excised human skin. Additional in vitro studies were performed in order to evaluate, after UVA radiation treatment, the spectral stability of the sunfilters once formulated in NLC or NE. From the results obtained, when incorporated in NLC, the skin permeation abilities of the sun filter were drastically reduced, remaining mainly on the surface of the skin. The photostability studies showed that EHT, DHHB and Tinosorb S still retain their photostability when incorporated in these carriers, while OMC and AVO were not photostable as expected. However, no significant differences in terms of photoprotective efficacy between the two carriers were observed.
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Portadores de Fármacos/química , Lípidos/química , Nanoestructuras/química , Protectores Solares/química , Protectores Solares/farmacología , Rayos Ultravioleta/efectos adversos , Química Farmacéutica/métodos , Estabilidad de Medicamentos , Humanos , Tamaño de la Partícula , Permeabilidad , Piel/metabolismo , Absorción Cutánea/fisiologíaRESUMEN
Lipid nanoparticles (LN) are drug carriers possessing advantages with respect to stability, drug release profile, and biocompatibility. There are several production methods for lipid nanoparticles. Recently high shear homogenization (HSH) and ultrasound (US) techniques have been used to produce these systems in a cheaper and easier way. The objective of the present study was to evaluate the effect of same important instrumental parameters, such as homogenization time (HT) and ultrasonication time (UT), on particle size (MD) and polydispersity index (PDI) of LNs obtained by HSH-US techniques. Curcumin was used as a model drug to be incapsulated in the LNs. LN were prepared by HSH-US technique using tripalmitin (Dynasan 116) and poloxamer 188 (Lutrol F68) as solid lipid and surfactant, respectively. The preparations were characterized and then evaluated using a factorial design study. From the results obtained, LNs produced by HSH-US method were characterized by nanodimension, high homogeneity and encapsulation efficiency. US technology plays an important role in controlling the final dimension of LN dispersion, while longer times of HSH seem mainly to exert a positive effect on the final homogeneity of particle dispersion. Additional studies are in progress to evaluate drug release profile from LNs, for further in vitro/in vivo correlation studies.
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Curcumina/química , Lípidos/química , Nanopartículas , Ultrasonido , Rastreo Diferencial de CalorimetríaRESUMEN
The aim of this study was to assess the ability of some vehicles (emulsion and emulgel), containing hydrogenated lecithin as penetration enhancer, in increasing the percutaneous absorption of the two model compounds dipotassium glycyrrhizinate (DG) and stearyl glycyrrhetinate (SG). Furthermore SG-loaded solid lipid nanoparticles (SLNs) were prepared and the effect of this vehicle on SG permeation profile was evaluated as well. Percutaneous absorption has been studied in vitro, using excised human skin membranes (i.e., stratum corneum epidermis or [SCE]), and in vivo, determining their anti-inflammatory activity. From the results obtained, the use of both penetration enhancers and SLNs resulted in being valid tools to optimize the topical delivery of DG and SG. Soy lecithin guaranteed an increase in the percutaneous absorption of the two activities and a rapid anti-inflammatory effect in in vivo experiments, whereas SLNs produced an interesting delayed and sustained release of SG.
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Antiinflamatorios/farmacología , Ácido Glicirretínico/análogos & derivados , Ácido Glicirrínico/farmacología , Lecitinas/metabolismo , Administración Tópica , Adulto , Antiinflamatorios/metabolismo , Portadores de Fármacos , Emulsiones , Eritema/tratamiento farmacológico , Eritema/etiología , Eritema/patología , Femenino , Geles , Ácido Glicirretínico/metabolismo , Ácido Glicirretínico/farmacología , Ácido Glicirrínico/metabolismo , Humanos , Hidrogenación , Masculino , Nanopartículas , Tamaño de la Partícula , Permeabilidad , Piel/efectos de los fármacos , Piel/metabolismo , Piel/patología , Absorción Cutánea , Rayos Ultravioleta/efectos adversosRESUMEN
The aim of the present work was to evaluate the antioxidant and photoprotective effect of blanch water (BW), a byproduct of the almond processing industry. The polyphenolic content of a BW extract, the level of proanthocyanidins and the vanillin index determination were determined. The antioxidant activity and the radical scavenging activity of the BW were evaluated by a range of in vitro tests. The in vivo photoprotective effect was investigated using a formulation containing 2% of the BW extract on skin erythema induced by acute UV-B exposure in twelve volunteers. Results confirmed the presence of added-value antioxidant compounds in the industrial BW extract, and the most representative compounds were naringenin-7-O-glucoside and kaempferol-7-O-rutinoside. The proanthocyanidin content was 71.84 ± 5.21 cyanidin equivalents/g of BW extract. The good antiradical activity of the BW extract was demonstrated in both the DPPH⢠test and in the Reducing Power test. The percentage inhibition of erythema obtained using a formulation of BW was 50.48, value clearly demonstrating an effect against photooxidative damage in vivo.
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Depuradores de Radicales Libres/química , Nueces/química , Extractos Vegetales/química , Prunus/química , Protectores contra Radiación/química , Aguas Residuales/química , Compuestos de Bifenilo/química , Eritema/etiología , Eritema/prevención & control , Industria de Procesamiento de Alimentos , Depuradores de Radicales Libres/aislamiento & purificación , Depuradores de Radicales Libres/farmacología , Radicales Libres/química , Humanos , Picratos/química , Extractos Vegetales/aislamiento & purificación , Extractos Vegetales/farmacología , Traumatismos por Radiación/etiología , Traumatismos por Radiación/prevención & control , Protectores contra Radiación/aislamiento & purificación , Protectores contra Radiación/farmacología , Piel/efectos de los fármacos , Piel/patología , Piel/efectos de la radiación , Rayos Ultravioleta/efectos adversosRESUMEN
Nocellara del Belice, a cultivated variety (cultivar) of olive tree (Olea europæa L.), was examined with respect to the medium-polar compounds present in the wastewaters of olive oil extraction at the end of 2007. Charcoal-polyamide chromatography of obtained wastewaters showed the presence of the chemotaxonomical markers of Olea europaea. In addition a new compound was isolated which resulted to be a lactone related to oleuropein aglycone. We propose the name of nocellaralactone (NOC). This compound is also present in the leaves and it appears to be structurally, probably biogenetically, related to jasminanhydride, a monoterpenoid previously isolated from Jasminum grandiflorum. NOC showed a significant in vitro anti-inflammatory activity.