Urea incorporated into ordered mesoporous silica for potential cosmetic application

Urea's thermal instability and burning on sensitive skin can cause problems for cosmetic formulations. To overcome these drawbacks, urea was incorporated into ordered mesoporous silica (SBA-15). SBA-15 was synthesized using tetraethyl orthosilicate and Pluronic® P123 in an acid medium. Urea (20 wt.%) was incorporated into calcined SBA-15 by the incipient wetness impregnation method. Several techniques were used to characterize the samples. Skin hydration and transepidermal water loss were measured using Corneometer® CM 825 PC and Tewameter® 300 TM. Results showed that the structural properties of SBA-15Urea were similar to pure SBA-15, indicating that SBA-15 remained structured even after urea incorporation. Nitrogen physisorption data showed the volume and surface area of the pores in SBA-15Urea were much lower than those in SBA-15, demonstrating that urea was deposited inside the mesopores. In vivo moisturization studies revealed that SBA-15Urea was not able to reduce transepidermal water loss compared to the other products and control, while forming a non-occlusive surface film on the skin. We conclude that incorporation of urea in the pores of the inorganic SBA-15 matrix is a promising approach to enhancing its stability and providing a prolonged moisturizing effect.

Low density lipoprotein modified silica nanoparticles loaded with docetaxel and thalidomide for effective chemotherapy of liver cancer

In the present study, we successfully developed a docetaxel (DTX) and thalidomide (TDD) co-delivery system based on low density lipoprotein (LDL) modified silica nanoparticles (LDL/SLN/DTX/TDD). By employing the tumor homing property of LDL and the drug-loading capability of silica nanoparticles, the prepared LDL/SLN/DTX/TDD was expected to locate and specifically deliver the loaded drugs (DTX and TDD) to achieve effective chemotherapy of liver cancer. In vitro analysis revealed that nano-sized LDL/SLN/DTX/TDD with decent drug loading capabilities was able to increase the delivery efficiency by targeting the low density lipoprotein receptors, which were overexpressed on HepG2 human hepatocellular liver carcinoma cell line, which exerted better cytotoxicity than unmodified silica nanoparticles and free drugs. In vivo imaging and anti-cancer assays also confirmed the preferable tumor-homing and synergetic anti-cancer effects of LDL/SLN/DTX/TDD.

Avaliação de protetores solares contendo filtros encapsulados/incorporados em matriz de sílica mesoporosa ordenada do tipo SBA-15 / Evaluation of sunscreens containing encapsulated/entrapped UV filters in ordered mesoporous silica type SBA-15

Filtros orgânicos são amplamente utilizados em formulações fotoprotetoras, com habilidade de absorver radiações ultravioleta (UV). Contudo, parte destes compostos possuem limitações, como: fotoinstabilidade, permeação cutânea e fotossensibilização e entre outros. Este trabalho envolveu a síntese de matriz mesoporosa do tipo SBA-15, encapsulação/incorporação de ρ-metoxicinamato de octila (MCO), benzofenona-3 (BZF-3) e avobenzona (AVO) na SBA-15 para aplicação em formulações fotoprotetoras. Fez-se a determinação da eficácia in vitro dos filtros encapsulados/incorporados combinados a ingrediente cosmético; o preparo de bastão fotoprotetor e determinação eficácia estimada; a avaliação do potencial de irritação ocular dos bastões por HET-CAM - Hen's Egg Test - Chorioallantoic Membrane, e a avaliação da permeação/retenção cutânea e perfil de biodistribuição dos filtros. Para a caracterização dos materiais foram empregadas técnicas físico-químicas e analíticas. As medidas de adsorção/dessorção de N2 mostrou que as amostras dos filtros solares encapsulados/incorporados apresentaram diminuição na área superficial e volume de poro (V), indicando que os filtros solares foram encapsulados/incorporados na superfície e nos poros da SBA-15. Os resultados de Espalhamento de raios X a baixo ângulo evidenciaram que os filtros solares não afetaram a estrutura hexagonal da SBA-15. Por TG/DTG e análise elementar foi possível determinar a quantidade de filtros solares na superfície e nos mesoporos da SBA-15. Enquanto, as curvas DSC e DTA revelaram aumento na estabilidade térmica da AVO e BZF-3, quando encapsulados/incorporados. Os resultados da eficácia fotoprotetora in vitro mostraram que a combinação dos três filtros solares encapsulados/incorporados na SBA-15 promoveram aumento de 52% no fator proteção solar (FPS), enquanto que, na formulação fotoprotetora contendo os três filtros encapsulados/incorporados, o aumento foi de 94%. O ensaio de HET-CAM evidenciou que os bastões contendo SBA-15 e os filtros encapsulados/incorporados não foram irritantes. O ensaio de permeação/retenção cutânea mostrou que o processo de encapsulação/incorporação da BZF-3 promoveu diminuição de sua permeação em todos os tempos de exposição. As quantidades permeadas de AVO e MCO ficaram abaixo do limite de quantificação nos tempos 6 e 12 h, no entanto, no tempo de 24 h foi possível quantificá-los. As quantidades dos filtros solares retidas na pele a partir da formulação contendo os filtros solares encapsulados/incorporados na SBA-15 (F4) foram menores (tempos 6 e 12 h) em comparação à formulação contendo os filtros solares não encapsulados (F3). A investigação da biodistribuição dos filtros solares mostrou que a retenção total na pele, como na derme, foi menor na formulação F4 em comparação à F3. O estudo comparativo entre pele suína e a pele humana mostrou que as quantidades de BZF-3 e AVO permeadas e retidas na pele suína foram superiores do que em relação à humana para ambas as formulações (F4 e FR). Pela técnica de biodistribuição, foi possível determinar que os filtros solares oriundos das formulações F3 e referência (FR) apresentaram maior retenção destes compostos na derme do que em outras camadas da pele. Contudo, observou-se que os filtros encapsulados apresentaram taxa reduzida de retenção na derme

Organic Filters are chemical compounds widely used in sunscreens formulations with the ability to absorb ultraviolet radiation (UV). Despite the effectiveness of these compounds in UV radiation protection, disadvantages related to their photo instability, potential skin permeation and photo sensibility pose significant challenges for improving these products. The aim of this work was to synthesize mesoporous matrix SBA-15, encapsulation/entrapping of octyl methoxycinnamate (OMC), benzophenone-3 (BZF-3) and avobenzone (AVO) into SBA-15 for application in photoprotective formulations. It was accessed in vitro photoprotection efficacy and in vitro photostability assay of encapsulated/entrapped UV filters combined with cosmetic ingredient and photoprotective stick formulations; evaluation of the ocular irritation potential of photoprotective stick formulations by in vitro method HET-CAM - Hen's Egg Test - Chorioallantoic Membrane; evaluation the skin permeation/deposition and biodistribution profile of photoprotective stick formulations. The decrease in the surface area and in mesoporous volume (V) observed in the nitrogen adsorption desorption isotherms of encapsulated/entrapped samples indicated that UV filters were efficiently encapsulated/entrapped into SBA-15. Additionally, SAXS results showed that UV filters did not affected the hexagonal structure of the mesoporous material and that these compounds filled the SBA-15 pores. TG/DTG and elemental analysis were efficient tools to confirm the presence and the quantity of UV filters into SBA-15. DTA and DSC curves of encapsulated/entrapped materials showed that the thermal stability of AVO and BZF-3 were increased. On the other hand, DSC curves of encapsulated/entrapped materials demonstrated that thermal stability of OMC was not increase. The in vitro photoprotective efficacy results demonstrated that the combination of the three sunscreens encapsulated/entrapped into SBA-15 increased 52.0% the SPF values, while the stick formulation containing the UV filters encapsulated/entrapped, the increase was 94.0%. Delivery experiments using porcine skin demonstrated that the encapsulation/entrapping process of UV filters resulted the decreased of BZF-3 permeation and deposition in skin (6 and 12 hours). The cutaneous biodistribution profile of UV filters showed that the deposition of these compounds from encapsulated/entrapped stick formulation (F4) was significantly lower than that from UV filters stick formulations (F3) in the total slices of the skin and dermis. The comparative study between porcine skin and human skin demonstrated that the amounts of BZF-3 and AVO permeated and deposited in porcine skin were higher than in human skin for both formulations (F4 and FR - reference formulation). By the biodistribution technique it was possible to determine that the UV filters from the formulations F3 and FR presented higher retention of these compounds in the dermis than in other layers of the skin. On the other hand, it was observed that the encapsulated UV filters presented low retention rate into dermis

Eficacia de un dentífrico con dióxido de silicio obliterante en pacientes con hiperestesia dentinaria / Efficacy of a toothpaste containing precipitated silica particles in patients with dentin hyperesthesia

Introducción: la hiperestesia dentinaria se caracteriza por un dolor intenso y breve asociado a la exposición de estímulos térmicos, táctiles, osmóticos o químicos. De prevalencia creciente, reduce la calidad de vida del paciente. Objetivo: evaluar la eficacia, aceptabilidad y tolerancia de un dentífrico con dióxido de silicio obliterante, nitrato potásico y monofluorofosfato sódico en pacientes con hiperestesia dentinaria. Métodos: estudio observacional y longitudinal (n= 22) en el que se aplicó el dentífrico 3 veces/día durante 28 días. Se realizó una evaluación clínica, antes y después de la aplicación, a las 48 horas, a las 96 horas y los días 7, 14, 21 y 28 del estudio. Se evaluó su eficacia en términos de reducción de la hipersensibilidad dental determinada mediante técnica táctil (escala de calificación verbal) y de chorro de aire (escala de Schiff). En cada visita se valoró la tolerancia del producto. Los pacientes valoraron el grado de hipersensibilidad y su percepción del producto mediante un cuestionario de evaluación subjetiva. El estudio se realizó bajo los principios de Buena Práctica Clínica. Resultados: la hipersensibilidad dental se redujo en todos los puntos temporales del estudio y fue significativa (p< 0,05) a partir del día 5. Esta mejoría fue sostenida y aumentó a medida que avanzó el tratamiento. El día 29 la hipersensibilidad media se redujo en un 85 por ciento respecto al valor basal en todos los pacientes. El 91 por ciento de los participantes opinó que el dentífrico había cumplido sus expectativas. No se observó ninguna reacción adversa derivada del uso del producto. Conclusiones: el dentífrico, administrado 3 veces/día, consiguió una reducción de la hipersensibilidad dental, significativa a partir del día 5, que fue aumentando con el tiempo. El producto presentó muy buena aceptabilidad y tolerancia(AU)

Introduction: dentin hypersensitivity is characterized by sharp pain of short duration associated with exposure to thermal, tactile, osmotic or chemical stimuli. Dentin hypersensitivity is a disorder of growing prevalence which reduces the quality of life of patients. Objective: evaluate the efficacy, acceptability and tolerance of a toothpaste with precipitated silica, potassium nitrate and sodium monofluorophosphate in patients with dentin hypersensitivity. Methods: an observational longitudinal study was conducted (n= 22) in which the toothpaste was applied 3 times a day for 28 days. Clinical assessment was performed before and after the application, at 48 hours, at 96 hours and on days 7, 14, 21 and 28 of the study. Efficacy was evaluated in terms of dental hypersensitivity reduction as determined by tactile (Verbal Rating Scale) and air jet (Schiff scale) techniques. Tolerance to the product was assessed in every visit. Patients ranked the degree of hypersensitivity and their perception of the product by means of a subjective assessment questionnaire. The study complied with Good Clinical Practice principles. Results: areduction was observed in dental hypersensitivity at all time points throughout the study, and it was significant (p< 0,05) as of day 5. This improvement was sustained and increased as treatment progressed. On day 29 mean hypersensitivity had reduced 85 percent with respect to baseline value in all patients. 91 percent of the patients stated that the toothpaste had met their expectations. No adverse reaction attributable to the product was observed. Conclusions: applied 3 times/day, the toothpaste obtained a reduction in dental hypersensitivity, which was significant as of day 5. This improvement increased over time. The product had very good acceptability and tolerance(AU)

Trastuzumab-Conjugated Liposome-Coated Fluorescent Magnetic Nanoparticles to Target Breast Cancer

OBJECTIVE: To synthesize mesoporous silica-core-shell magnetic nanoparticles (MNPs) encapsulated by liposomes (Lipo [MNP@m-SiO2]) in order to enhance their stability, allow them to be used in any buffer solution, and to produce trastuzumab-conjugated (Lipo[MNP@m-SiO2]-Her2Ab) nanoparticles to be utilized in vitro for the targeting of breast cancer. MATERIALS AND METHODS: The physiochemical characteristics of Lipo[MNP@m-SiO2] were assessed in terms of size, morphological features, and in vitro safety. The multimodal imaging properties of the organic dye incorporated into Lipo[MNP@m-SiO2] were assessed with both in vitro fluorescence and MR imaging. The specific targeting ability of trastuzumab (Her2/neu antibody, Herceptin(R))-conjugated Lipo[MNP@m-SiO2] for Her2/neu-positive breast cancer cells was also evaluated with fluorescence and MR imaging. RESULTS: We obtained uniformly-sized and evenly distributed Lipo[MNP@m-SiO2] that demonstrated biological stability, while not disrupting cell viability. Her2/neu-positive breast cancer cell targeting by trastuzumab-conjugated Lipo[MNP@m-SiO2] was observed by in vitro fluorescence and MR imaging. CONCLUSION: Trastuzumab-conjugated Lipo[MNP@m-SiO2] is a potential treatment tool for targeted drug delivery in Her2/neu-positive breast cancer.

Evaluation of some biological aspects of the presence of abrasive silica and thickening silica in basic formulations of dentifrices / Evaluación de algunos aspectos biológicos de la presencia de sílice abrasivo y sílice espesante en formulaciones básicas de dentífricos

The aim of this study was to evaluate some biological characteristics and toxicity of basic formulations of dentifrices containing such substances, and to compare them with two existing products in market which also contains silic in their formulations. In this way, it was evaluated some biological parameters: weight of the animals, oral toxicity, hematological parameters, urinary analysis, and histological evaluation. The thrombocytes were also statistically at normal levels. The glutamate-pyruvate transaminase (TGP) showed normal aspect in 5 of the tested groups, as in control. Meanwhile, the oxalacetic transaminase (AST) in one group had a small increase in the control group. Regarding urine, in exception the rats of one group, the rats of the 4 other experimental groups showed leukocytosis urinary statistically higher than the control group. The histological evaluation of the animals showed that specimens from liver, stomach, kidney and submandibular gland presented normal aspects for these organs, without significant characteristics related to inflammatory infiltrates in any of the 6 samples tested in their respective groups.

El objetivo del estudio fue evaluar algunas características biológicas y de toxicidad provenientes de las formulaciones básicas de dentífricos que contienen sílice en su composición y compararlos con dos dentífricos disponibles comercialmente que también presentan sílice. El análisis hematológico no mostró diferencias entre los grupos evaluados. Los niveles de trombocitos presentados por los grupos fueron también normales. La transaminasa gluámico pirúbica se mostró un aspecto normal en 5 de los grupos estudiados, así como en el grupo control. La transaminasa glutámico oxaloacética en uno de los grupos tuvo un pequeño incremento. En relación a la orina, 4 grupos presentaron leucocitosis urinaria significativamente mayor que el grupo de control. La evaluación histológica del hígado, estómago, riñones y glándulas submandibulares se presentó con aspecto normal, sin presencia de infiltrado inflamatorio.

pH-cycling models to evaluate the effect of low fluoride dentifrice on enamel de- and remineralization

Since the currently available pH-cycling models do not differentiate the anti-caries potential of dentifrices with low fluoride (F) concentration, two models were developed and tested in the present. Bovine enamel blocks were subjected to the models and treated with F solutions containing from 70 to 280 mug F/mL in order to validate them in terms of dose-response effect. The models were also tested by evaluating the dentifrices Colgate Baby (500 mug F/g, as a low fluoride dentifrice), Tandy (1,100 mug F/g, as an active F-dentifrice) and Crest (1,100 mug F/g, as positive control). Enamel mineral loss or gain was assessed by surface and cross-sectional microhardness, and lesion depth was analyzed by polarized light microscopy. The pH-cycling models showed F dose-response effect either reducing enamel demineralization or enhancing remineralization. The low F dentifrice presented anti-caries potential, but it was not equivalent to the dentifrices containing 1,100 mug F/g. These data suggest that the models developed in this study were able to evaluate the anti-caries potential of low F dentifrice either on resistance to demineralization or on enhancement of remineralization.

Tendo em vista que os modelos atuais de ciclagens de pH não diferenciam o potencial anti-cárie de dentifrícios com baixa concentração de fluoreto (F), dois modelos foram desenvolvidos e testados. Blocos de esmalte bovino foram submetidos aos modelos e tratados com soluções de concentrações crescentes de F (70 a 280 mig F/mL) para validar os modelos em termos de dose-resposta. A seguir, os modelos foram testados avaliando o potencial anti-cárie dos dentifrícios Colgate Baby (500 mig F/g, dentifrício de baixa concentração), Tandy (1.100 mig F/g, como controle ativo) e Crest (1.100 mig F/g, como controle positivo). Perda ou ganho de mineral pelo esmalte foi avaliada por microdureza e profundidade de lesão de cárie foi avaliada por microscopia de luz polarizada. Os modelos de ciclagens de pH desenvolvidos mostraram efeito do F dose-resposta quer seja na redução da desmineralização como na remineralização do esmalte. O dentifrício de baixa concentração de F mostrou ter potencial anti-cárie, o qual não foi equivalente aos dentifrícios contendo 1.100 mig F/g. Os resultados sugerem que os modelos desenvolvidos são capazes de avaliar o potencial anti-cárie de dentifrício de concentração reduzida de F, quer seja na sua capacidade de aumentar a resistência do esmalte a desmineralização como na ativação da remineralização.

Nitric oxide production by rat bronchoalveolar macrophages or polymorphonuclear leukocytes following intratracheal instillation of lipopolysaccharide or silica.

Exposure of the lung to lipopolysaccharide (LPS) or silica results in an activation of alveolar macrophages (AMs), recruitment of polymorphonuclear leukocytes (PMNs) into bronchoalveolar spaces, and the production of free radicals. Nitric oxide (NO) is one of the free radicals generated by bronchoalveolar lavage (BAL) cell populations following either LPS or silica exposure. The purpose of the present study was to assess the relative contributions of AMs and PMNs to the amounts of NO produced by BAL cells following intratracheal (IT) instillation of either LPS or silica. Male Sprague Dawley rats (265-340 g body wt.) were given LPS (10 mg/100 g body wt.) or silica (5 mg/100 g body wt.). BAL cells were harvested 18-24 h post-IT and enriched for AMs or PMNs using density gradient centrifugation. Media levels of nitrate and nitrite (NOx; the stable decomposition products of NO) were then measured 18 h after ex vivo culture of these cells. Following IT exposure to either LPS or silica, BAL cell populations were approximately 20% AMs and approximately 80% PMNs. After density gradient centrifugation of BAL cells from LPS- or silica-treated rats, cell fractions were obtained which were relatively enriched for AMs (approximately 60%) or PMNs (approximately 90%). The amounts of NOx produced by the AM-enriched fractions from LPS- or silica-treated rats were approximately 2-4-fold greater than that produced by the PMN-enriched fractions. Estimations of the relative contribution of AMs or PMNs to the NOx produced indicated that: (i) following LPS treatment, 75%-89% of the NOx was derived from AMs and 11%-25% from PMNs; and (ii) following silica treatment, 76%-100% of the NOx was derived from AMs and 0-24% from PMNs. Immunohistochemistry for inducible NO synthase on lung tissue sections supported these findings. We conclude that AMs are the major source of the NO produced by BAL cells during acute pulmonary inflammatory responses to LPS or silica.

Efecto antiinflamatorio del líquido amniótico en el pulmón de ratas inoculadas intratraquealmente con sílice / Antiinflamatory efect of amniotic fluid in the lung of ratas intratracheally inoculated with silica

El síndrome de aspiración de meconio representa un estado patológico de gran importancia para la medicina humana; sin embargo, es poco conocido en medicina veterinaria. En los últimos años se han realizado varias investigaciones con el fin de esclarecer la importancia y patogénesis de este síndrome en los animales domésticos. Estudios recientes han surgido un posible efecto antiinflamatorio del líquido amniótico debido a que la aspiración de este líquido contaminado con queratina, la cual es un factor proinflamatorio, sólo induce una respuesta inflamatoria leve en el pulmón de becerros. El objetivo de esta investigación fue determinar si el líquido amniótico produce un efecto antiinflamatorio en los pulmones de ratas inoculadas intratraquealmente con sílice. Treinta y ocho ratas Wistar de 177 g en promedio se dividieron en cinco grupos. Cada grupos recibió vía intratraqueal diferentes dosis de líquido amniótico y solución salina fisiológica (0, 0.125, 0.250, 0.375 y 0.5 ml, respectivamente) y cantidades constantes de sílice (5 mg/ml). Los animales inoculados se sacrificaron a las 72 horas posinoculación y se realizaron lavados broncoalveolares. Se realizó la cuenta total de células nucleadas por ml de lavado, así como el porcentaje y cuenta absoluta de neutrófilos y macró fagos. La inoculación con sílice y líquido amniótico indujo un marcado incremento en la cuenta total de células nucleadas y en el número de neutrófilos (P < 0.01) en los grupos tratados respecto del testigo. El incremento se mostró como una función directa del volumen de líquido amniótico inoculado. Sin embargo, se concluyó que el líquido amniótico no tuvo un efecto antiinflamatorio en el pulmón de ratas inoculadas intratraquealmente con sílice

Effectiveness of slow release formulations of fenthion (Baytex) in the control of Mansonia breeding in polluted pond habitats.

Effectiveness of two types of granular formulations of fenthion (Baytex) was evaluated in controlling the breeding of Mansonia mosquitos in polluted pond habitats. Calcium carbonate and sand granular formulations, when applied at 2.50 g/m2 surface area with an average depth of 0.5 m were found to be effective in keeping the habitats completely free from Mansonia breeding for 14 days and 18 days respectively. Release of insecticide was slow and the effective duration of control after a single application was relatively longer in the sand formulation when compared to the calcium carbonate formulation. Single application of calcium carbonate and sand granular formulations of fenthion could effectively prevent Mansonia adult emergence for 23 and 30 days, respectively in polluted pond habitats, without causing any adverse effect on non-target insects.