Compounded Orodispersible Films with Natural Ingredients for Halitosis: A Clinical Experience.

Halitosis can be described as unpleasant odors emanating from the oral cavity. It is usually associated with decomposition action of bacteria present mainly on the back of the tongue and periodontal pockets, and able to produce volatile sulfur compounds. We conducted a study at the Faculty of Dentistry, Federal University of Juiz de Fora and evaluated the therapeutic effect of two natural extracts, Camellia sinensis (green tea) and resveratrol in the form of oral polymer films, to control halitosis. Fifty volunteers (students of health courses) participated in the research after orientation and signing the informed consent form. The anamnesis was made by researchers. The physical examination was made to verify the inclusion criteria. Each participant received 45 polymeric films to be consumed in 15 days (3 films per day). Measurements of the volatile sulfur compound levels were performed using a halimeter in two stages: 1) before use and 2) 15 days after the first administration. Results showed a statistically significant reduction in volatile sulfur compound levels in 71.79% of the volunteers. We concluded that the compounded orodispersible films containing green tea and resveratrol demonstrated excellent results in reducing halitosis.

Delivering Resveratrol on the Buccal Mucosa Using Mucoadhesive Tablets: A Potential Treatment Strategy for Inflammatory Oral Lesions.

BACKGROUND: Resveratrol is a polyphenol that has gained momentum in therapeutics in the last few years. OBJECTIVE: In this study, we hypothesised that resveratrol could act prophylactically and/or treat inflammatory lesions of the oral cavity after being delivered by two different formulations of buccal mucoadhesive tablets (F1 and F2, which differed in terms of viscosity agents used). METHODS: This hypothesis was assessed through permeation studies, to verify diffusion of the drug through the buccal mucosa using a porcine model to predict human in vivo behaviour. RESULTS: F2 (tablet with less viscosity agent) presented better permeation than F1, but the amount of drug that crossed the mucosa was still low compared to the amount retained within it (35.90 µg found in the receptor medium and 15.63 mg quantified within the mucosa). CONCLUSION: This accounted for a local effect rather than a systemic one, which is desirable for local processes, such as oral mucositis, lichen planus, erythema multiforme, nicotinic stomatitis, recurrent aphthous stomatitis, among others. In this sense, resveratrol-loaded mucoadhesive tablets appear to be a prominent alternative to prevent and/or cure inflammatory lesions of the oral cavity.

Technological Device for Manufacturing Transdermal Films: Possible Applications to the Individualized Treatment for Erectile Dysfunction.

Pharmacological advances in erectile dysfunction (ED) treatment have aroused growing interest among health professionals towards sexual dysfunction, generating an increasing demand for dosage forms and drug delivery systems, including tadalafil. This study aimed to develop a device to generate patches that would enable drug dosage individualization and transdermal administration. To create such a mechanical device, technical drawings were made using the CAD software. A functional prototype was built, and a pharmaceutical formulation containing tadalafil (10 mg cm-2) was prepared. An analytical method (HPLC) was developed and validated. The average weight of adhesives (n = 10) was 241.01 mg; the content uniformity for preparations in unit doses (n = 10) was 108.93%, and a CV <2% for intraadhesive tadalafil content (n = 40) was observed. The ex vivo permeation of patches containing tadalafil was determined in Franz cells (n = 6), equipped with human skin and kept for 12 h in contact with the patch, by using the tape stripping method. The optimized method showed acceptable confidence limits within the range recommended by regulatory agencies, being validated for use in this ex vivo permeation study. Tadalafil could permeate to the viable epidermis and dermis (5.7%). The created device produced homogeneous patches of tadalafil, showing such technological innovation as to be feasible in individualized therapy for the treatment of ED.

Ex vivo Skin Permeation Evaluation of An Innovative Transdermal Vehicle Using Nimesulide and Piroxicam as Model Drugs.

BACKGROUND: The transdermal dosage forms presented a limited usage for a long time, for it was believed that the stratum corneum, the outermost layer of epidermis, made it impracticable the permeation of medications through the skin. Studies exploring this area came up with strategies to overcome this barrier; for example, creating a transdermal vehicle to facilitate the drug absorption. OBJECTIVE: This study aimed to evaluate a new transdermal vehicle through the comparison of its permeation profile and the profile of commercial products, using nimesulide and piroxicam, non steroidal anti-inflammatory drugs. METHODS: Four different products were evaluated: nimesulide and piroxicam compounded with the new vehicle (emulsion) and commercial nimesulide and piroxicam gels. Ex vivo permeation experiments using Franz-type diffusion cell equipment were conducted, using human skin as membrane. For evaluation of permeated active pharmaceutical ingredients concentrations, we performed quantification from the receptor solution, stratum corneum and viable epidermis + dermis, through high-performance liquid chromatography analyses. RESULTS: The new vehicle promoted increased permeation of active pharmaceutical ingredients through the viable epidermis and dermis, when compared to commercial products, but the stratum corrneum continued to keep the highest retention. CONCLUSION: The innovative vehicle was capable of enhancing the transdermal absorption of active pharmaceutical ingredients from the compounded formulations, thus, demonstrating the capability thereof to improve the permeability of active pharmaceutical ingredients by transdermal use.

Prevalências de doenças de grande impacto na saúde pública em idosos frágeis residentes na Zona da Mata Mineira-Brasil: um estudo de base populacional / Prevalence of major Public Health impact diseases among frail elderly residents in the Zona da Mata region in the state of Minas Gerais-Brazil: a population-based study

O objetivo deste estudo transversal, descritivo, observacional e de base populacional foi identificar as prevalências de certas doenças de elevado custo e impacto no setor de Saúde Pública e de alguns hábitos de vida de idosos frágeis residentes na zona da Mata Mineira (Brasil). A pesquisa envolveu 7.113 idosos frágeis, de ambos os sexos, com idade igual ou superior a 60 anos. As informações foram obtidas, a partir do banco de dados eletrônico mantido e organizado pelo Centro Mais Vida. Observou-se um maior número de idosos do sexo feminino (67,6%), com idade entre 60 a 69 anos (40,4%) e casados (48,5%). 9,3% da população pesquisada apresentavam comprometimento cognitivo leve, 11,8% incapacidade cognitiva, 5,0% depressão, 9,0% demências, 7,9% insuficiência cardíaca, 21,6% diabetes Mellitus, 44,5% dislipidemias. Quanto aos hábitos de vida, 69,6% eram sedentários, 11,1% fumavam tabaco e 2,7% eram etilistas. Esses dados permitem comparações em nível internacional e são essenciais para a elaboração de políticas efetivas e intervenções primárias, secundárias e terciárias a nível populacional.

This cross-sectional, descriptive, observational and population-based study aimed to identify the prevalence of costly diseases and their impact on the public health sector, as well as lifestyle habits of frail elderly residents in Zona da Mata, Minas Gerais (Brazil). The research involved 7,113 frail elderly of both genders, aged over 60 years. Data were obtained from the electronic database maintained and organized by the institution Centro Mais Vida. A greater number of frail elderly females (67.6%) aged from 60 to 69 years old (40.4%) and married (48.5%) was observed. 9.3% of the surveyed population had mild cognitive impairment, 11.8% had cognitive disability, 5.0% had depression, 9.0% had dementia, 7.9% had heart failure, 21.6% had diabetes Mellitus and 44.5% had dyslipidemia. For lifestyle, 69.6% were sedentary, 11.1% smoked tobacco and 2.7% were alcoholics. Such data allow comparisons at international level and are critical for the development of effective policies as well as primary, secondary and tertiary-level interventions among the population.

Permeation profiles of resveratrol cream delivered through porcine vaginal mucosa: Evaluation of different HPLC stationary phases.

Trans-resveratrol affects biological systems in a multitude of ways, but its oral bioavailability is remarkably poor due to in vivo metabolization. This drawback has fomented the development of new strategies for systemic delivery, such as transmucosal delivery via the vaginal route, which is our main focus here. In this sense, our pioneering study purposed to evaluate the trans-resveratrol permeation efficacy through this route. For that, we used a previously validated method and tested it with three different stationary phases: a commercial C18 column and two laboratory-made chromatographic columns containing poly(methyloctadecylsiloxane) (PMODS) thermally immobilized onto zirconized silica (Zr-PMODS) or titanized silica (Ti-PMODS). The permeation experiments showed that resveratrol, in the formulation used, was not successfully delivered to the bloodstream - it was actually retained within the vaginal mucosa, which suggests a local use rather a systemic one.

Synthesis of conjugated bile acids/azastilbenes as potential antioxidant and photoprotective agents.

A series of 14 bile acids/azastilbenes conjugates (1a-g and 2a-g) was prepared through the condensation of bile amides (1 and 2) and aromatic aldehydes. The newly synthesized conjugates were evaluated in vitro for their antioxidant and photoprotective activities. Six compounds (1, 1a, 1b, 2, 2a and 2b) showed promising antioxidant activity with IC50 values of 19.60-31.83 µg mL(-1). The synthesized compounds presented a varied photoprotection profile, with the SPF ranging from 2 to 9. Among the 16 compounds tested for the protection against UVB sunrays, 3 compounds (2c, 2e and 2g) presented more significant protection than resveratrol and the free azastilbene 3; while the UVAPF increased from 2 in resveratrol and 5 in 3 to 5-11 in the majority of the conjugates.

Studies with emulsion containing trans-resveratrol: in vitro release profile and ex vivo human skin permeation.

Resveratrol is a phenolic compound that has been widely studied in the last years because of its extensive pharmacological properties. It also has physicochemical properties that are adequate for diffusion through the human skin. An analytical method by high performance liquid chromatography was developed and validated for its determination in transdermal emulsion, as well in receptor media and skin layers. The trans-resveratrol release kinetic followed the Higushi's model (R(2) = 0.9926) with steady-state diffusion flux and lag time of 138.5 µg cm(-2) h(-1) and 0.49 h, respectively. It showed a percentage at 64.96 % for permeation. Thus, the results suggest that the emulsion studied is a potential vehicle for transresveratrol administration by transdermal route.

In vitro drug release and ex vivo percutaneous absorption of resveratrol cream using HPLC with zirconized silica stationary phase.

Since the designs of optimal formulations for resveratrol permeation via the skin are lacking, the aim of this study was to establish the profile of resveratrol permeability into and across human skin. For that, a laboratory-made chromatographic column was used (Zr-PMODS), with its performance being compared to a traditional C18 column. In vitro drug release was conducted with polysulfone membranes, and the flux (JS) was 30.49 µg cm(-2) h(-1)), with a lag time (LT) of 0.04 h, following a pseudo-first-order kinetics. For ex vivo percutaneous absorption using excised female human skin, the kinetic profile was the same, but JS was 0.87 µg cm(-2) h(-1) and LT was 0.97 h. From the initials 49.30 µg applied to the skin, 9.50 µg were quantified in the receptor medium, 20.48 µg was retained at the stratum corneum (do not account as permeated) and 21.41 µg was retained at the viable epidermis+dermis (account as permeated), totalizing 30.90 µg of resveratrol permeated after 24 h of application (62.6%). From these results, one can conclude that a person using the 1-g emulsion dose released by the pump containing 20mg of resveratrol will have, theoretically, 12.53 mg of it liberated into his bloodstream, gradually and continuously for 24 h.

Photoprotective activity of resveratrol analogues.

Resveratrol is a promising agent for protecting human skin from UV radiation and to reduce the occurrence of cutaneous malignancies. We describe the photoprotective activity of six resveratrol analogues using the diffuse transmittance technique to determine the SPF and the protection against UVA radiation. The analogues presented a varied profile of photoprotection, the SPF ranging from 2 to 10 and the UVAPF from 0 to 9. Among the six compounds tested, the protection against UVB sunrays provided by compound B was more significant than the protection provided by resveratrol; compounds C, D, E and F show photoprotection similar to resveratrol.

Fatty acid and phospholipase A2 plasma levels in children with autism.

OBJECTIVE: To evaluate fatty acid plasma levels, phospholipase A2 activity, and the developmental profiles of children with autism vs. control subjects. METHODS: Twenty four children with autism underwent laboratory analysis for fatty acid quantification using gas chromatography and PLA2 activity determination by fluorometric assay. RESULTS: No correlation was observed between the developmental quotient and fatty acid plasma levels. Phospholipase A2 activity was significantly higher among autistic children compared with controls. CONCLUSION: The study did not show a correlation between fatty acid and phospholipase A2 plasma levels and the developmental profile of children with autism.

Fatty acid and phospholipase A2 plasma levels in children with autism / Níveis plasmáticos de ácidos graxos e fosfolipase A2 em crianças com autismo

OBJECTIVE: To evaluate fatty acid plasma levels, phospholipase A2 activity, and the developmental profiles of children with autism vs. control subjects. METHODS: Twenty four children with autism underwent laboratory analysis for fatty acid quantification using gas chromatography and PLA2 activity determination by fluorometric assay. RESULTS: No correlation was observed between the developmental quotient and fatty acid plasma levels. Phospholipase A2 activity was significantly higher among autistic children compared with controls. CONCLUSION: The study did not show a correlation between fatty acid and phospholipase A2 plasma levels and the developmental profile of children with autism

OBJETIVO: Avaliar os níveis plasmáticos de ácidos graxos, a atividade da fosfolipase A2 e o perfil de desenvolvimento de crianças com autismo versus controles. MÉTODOS: Vinte e quatro crianças com autismo foram submetidas a exames laboratoriais para quantificação plasmática de ácidos graxos por cromatografia gasosa e para determinação da atividade de fosfolipase A2 por ensaio fluorimétrico. RESULTADOS: Nenhuma correlação foi observada entre o coeficiente de desenvolvimento e os níveis plasmáticos dos ácidos graxos quantificados. A atividade da fosfolipase A2 foi significativamente maior no grupo de crianças com autismo quando comparado ao grupo controle. CONCLUSÃO: O estudo não demonstrou correlação entre os níveis plasmáticos de ácidos graxos e fosfolipase A2 e o perfil de desenvolvimento de crianças com autismo

Low serum levels of 25-hydroxyvitamin D (25-OHD) in children with autism / Baixos níveis séricos de 25-hidroxivitamina D (25-OHD) em crianças com autismo

Objective: To confirm previous evidence suggesting an association between autism and low vitamin D serum levels. Methods: This preliminary exploratory study assessed the circulating levels of 25-hydroxyvitamin D (25-OHD) in pediatric patients with autism and in typically developing controls from Juiz de Fora, Brazil. Results: Serum levels of 25-OHD were lower in children with autism (26.48 ± 3.48 ng mL-1) when compared to typically developing subjects (40.52 ± 3.13 ng mL-1) (p < 0.001). Conclusion: Our findings attest to the importance of vitamin supplementation during pregnancy and in the treatment of children with autism, who tend to present low vitamin D consumption rates (AU)

Objetivo: Confirmar evidências prévias indicando uma associação entre autismo e baixos níveis séricos de vitamina D. Métodos: Este estudo preliminar avaliou os níveis circulantes de 25-hidroxivitamina D (25-OHD) em pacientes pediátricos com autismo e em controles apresentando desenvolvimento típico em Juiz de Fora, Brasil. Resultados: Os níveis séricos de 25-OHD foram menores em crianças com autismo (26,48 ± 3,48 ng mL-1) em comparação com indivíduos com desenvolvimento típico (40,52 ± 3,13 ng mL-1) (p < 0,001). Conclusão: Nossos resultados confirmam a importância da suplementação de vitamina durante a gravidez e no tratamento de crianças com autismo, que costumam apresentar um baixo consumo de vitamina D (AU)

Low serum levels of 25-hydroxyvitamin D (25-OHD) in children with autism.

OBJECTIVE: To confirm previous evidence suggesting an association between autism and low vitamin D serum levels. METHODS: This preliminary exploratory study assessed the circulating levels of 25-hydroxyvitamin D (25-OHD) in pediatric patients with autism and in typically developing controls from Juiz de Fora, Brazil. RESULTS: Serum levels of 25-OHD were lower in children with autism (26.48 ± 3.48 ng mL-1) when compared to typically developing subjects (40.52 ± 3.13 ng mL-1) (p < 0.001). CONCLUSION: Our findings attest to the importance of vitamin supplementation during pregnancy and in the treatment of children with autism, who tend to present low vitamin D consumption rates.

Mushroom tyrosinase inhibitory activity and major fatty acid constituents of Amazonian native flora oils

In order to treat hyperpigmentation-related problems, there has been a global trend in developing cosmetics claiming to have skin-whitening properties, which act by inhibiting melanin biosynthesis. The objective of this work was to evaluate the in vitro mushroom tyrosinase inhibitory activity of five Amazonian native flora oils, and so to verify the possibility of their incorporation into cosmetic products. In addition, the fatty acid composition of the essential oils was determined by gas chromatography-flame ionisation detection in order to determine the main components of these oils. The tyrosinase inhibitory activity of the tested oils was found to be in the following order: açaí (IA50 = 66.08 µg mL-1) > tucumã > patauá > pracaxi > castanha do Brasil. This study suggests that açaí oil has great potential in the treatment of hyperpigmentation and other related disorders, due to its considerable tyrosinase inhibitory activity.

Com o intuito de se tratar problemas dermatológicos de hiperpigmentação, há uma tendência mundial no desenvolvimento de cosméticos que possuam propriedades despigmentantes, os quais agem inibindo a biossíntese de melanina. O objetivo deste trabalho foi avaliar in vitro a atividade de inibição da tirosinase de cogumelo de cinco óleos de plantas nativas da Amazônia e, desta forma, verificar a possibilidade de sua incorporação em produtos cosméticos. Ainda, a composição de ácidos graxos dos óleos foi determinada por cromatografia gasosa com detecção por ionização de chama, no intuito de determinar os principais componentes destes óleos. A atividade de inibição da tirosinase dos óleos testados foi encontrada na seguinte ordem: açaí (IA50 = 66,08 µg mL-1) > tucumã > patauá > pracaxi > castanha do Brasil. Este estudo sugere que o óleo de açaí possui grande potencial para o tratamento da hiperpigmentação cutânea e doenças correlatas, devido à sua considerável atividade de inibição da tirosinase.

A terapia de reposição hormonal e a saúde da mulher no climatério: riscos e benefícios / Hormone replacement therapy and women's health during climacteric: risks and benefits

Embora esteja disponível há mais de seis décadas, a Terapiade Reposição Hormonal (TRH) é atualmente um tema controverso,na medida em que divide a comunidade científicaentre defensores e críticos, que exaltam tanto seus malefíciosquanto benefícios em igual proporção. Ao levantardiscussões que põem em xeque a sua própria importânciae a sua até então acreditada necessidade pela populaçãofeminina, mostra-se como assunto em evidência em diasatuais. Foi feito um levantamento de riscos e benefícios queesta terapia fornece, oferecendo dados para que médicos epacientes ponderem sobre sua utilização.

Fotoprotetores naturais como instrumento de ação primária na prevenção do câncer de pele / Natural sunscreens for primary prevention of skin cancer

Faz-se uma revisão explanatória acerca da implementação e utilização pela população de foto protetores, em especialos contendo ativos naturais, na profilaxia do câncer de pele.Esta patologia é uma importante questão de saúde pública brasileira e mundial, visto sua alta incidência em todos os estratos sociais. Seu principal fator desencadeador é aradiação ultravioleta proveniente do sol; por este motivo,a difusão, pela população, do uso contínuo e correto de foto protetores é uma medida fundamental de prevenção denovos casos. Aliado a isso, a busca por produtos naturaiscom elevadas eficácia, eficiência e segurança tem sido um grande esforço por parte de empresas e centros de pesquisa interessados, dada sua relevância no contexto das políticas públicas de desenvolvimento das potencialidades locais brasileiras.

This is an explanatory review of the implementation and use, by the general population, of sunscreens, especially those with natural active components, for protection against skin cancer. The latter is an important public health issue, in Brazil and worldwide, with high incidence rates in all social groups. Because the main associated risk factor is sun-derived ultraviolet radiation, the correct and continuous use of sun screens is a fundamental preventive measure. Furthermore, the search for natural and highly efficient, effective and safe products has been a target for the industry and research centers, motivated by the relevance of the issue for public policies contemplating the Brazilian potentialities.