Obtainment of the spray-dried extracts of Peperomia pellucida L. (H.B.K.) using different atomization temperatures: physicochemical characterization and technological development for pharmaceutical applications.

Spray-dried extracts are prepared as powders or granules after solvent removal, which can be obtained in the presence or absence of pharmaceutical adjuvants. This work aimed to optimize the process of obtaining dried extracts of Peperomia pellucida L. (HBK) by spray drying. The characterization of the extract was performed by thermal analysis, specific surface area, particle size and high performance liquid chromatography (HPLC); then, capsules were developed for antimicrobial treatment, evaluating four bench lots by the determination of the angle of repose and time of flow, scanning electron microscopy, porosity and physicochemical quality control. There were no significant differences between the extracts obtained by spray drying at atomization temperatures of 140 °C, 160 °C and 180 °C, which was confirmed by thermal analysis. Specific surface area varied inversely with the mean particle size. Regarding the marker content by HPLC, no significant differences were found between the samples, although the flavonoid fraction was more stable at 160 °C. Bench lots (I to IV) were developed using the diluents Flowlac®, Starch® 1500, microcrystalline cellulose 250 and Cellactose® 80. Based on the results, the bench lot I, containing Flowlac®, was selected. The results of physicochemical quality control demonstrated that the selected formulation meets the pre-established parameters, and proving to be economically viable.

Technological innovation strategies for the specific treatment of Chagas disease based on Benznidazole.

Caused by Trypanosoma cruzi, Chagas disease is responsible for public health problems greater in magnitude than those attributed to malaria, schistosomiasis, or leishmaniasis. A factor in the socioeconomic development of poor countries, Chagas disease can cause death due to a high parasitic burden during its acute phase due and irreversible damage in organs such as the heart, esophagus, and colon during its chronic phase, even when the number of parasites is minimal. For treating Chagas disease, benznidazole (BNZ) remains the drug of choice and, in Latin America, the only drug on the market for treating the disease. However, BNZ has exhibited insufficient activity in the chronic phase of Chagas disease, required administration in large doses, prolonged treatment, and shown a high incidence of adverse reactions (vomiting, rash, peripheral neuropathy, and spinal cord depression), toxicity, and low solubility in water. As an antidote, pharmaceutical technologies have been introduced that can improve BNZ's solubility and dissolution, as well as reduce side effects in light of its bioavailability, all of which can enhance therapy for Chagas disease. In response to that trend, by conducting a literature review, we sought to identify current pharmaceutical technologies used in tandem with BNZ to improve therapy for Chagas disease. Documented techniques include emulsion and microemulsion formation, solutions, parenteral formulas, micronization, and drug delivery systems supported by the development of nanoparticles and cyclodextrins, solid dispersions, and the use of metal-organic frameworks as innovative excipients. Such technologies increase the water solubility of BNZ by 4-25-fold on dissolution and an 85% release with efficacy in only a few minutes, as recorded during a viability experiment with nanoparticle suspensions. That experiment demonstrated the need for a lower concentration of BNZ to kill 50% of trypomastigote forms of T. cruzi, described in terms of the formation of BNZ-cyclodextrin complexes, and modulating and vectoring of the antichagasic by using metal-organic frameworks. Altogether, the promising results of research identified can enable strategies to improve solubility and efficacy of BNZ, as well as therapy for Chagas disease.

Avaliação da qualidade físico-química de formulações de álcoois em gel comercializadas na cidade de Irecê-Ba / Evaluation of the physicochemical quality of alcohol gel formulations selled in the city of Irecê-Ba / Evaluación de la calidad fisicoquímica de formulaciones de alcohol gel comercializadas en la ciudad de Irecê-Ba

Já é sabido que a higiene das mãos é a principal arma na prevenção de doenças infecciosas dentro e fora dos hospitais. No caso do vírus SARSCoV-2, a higienização das mãos é essencial, tendo em vista a possibilidade de contaminação pelo contato direto com as gotículas respiratórias ou pelo contato indireto. Existem no mercado diversas opções de produtos antissépticos disponíveis para uso pela população. No entanto, nenhum é 100% eficaz em todas as situações. Dentre esses diversos produtos disponíveis, o etanol 70% é o mais utilizado para a aplicação nas mãos, sendo veiculado na forma farmacêutica gel para facilitar a aplicação. As formas farmacêuticas gel contendo etanol 70% podem ser industrializadas ou manipuladas. Quando essas formulações são manipuladas, elas são isentas de registro na Agência de Vigilância Sanitária (ANVISA), não sendo exigidos nem mesmo os testes de segurança e eficácia que são exigidos para o registro de produtos industrializados. Para os manipulados, são realizados apenas os testes de descrição, aspecto, características organolépticas (cor e odor) pH e peso. Desta forma, a realização deste trabalho teve como objetivo avaliar a qualidade, incluindo características físico-químicas de amostras de álcool em gel manipuladas na cidade de Irecê-Ba, e compará-las com um produto industrializado de marca conhecida. Foram analisados os aspectos e características organolépticas, determinação do potencial de hidrogênio (pH), densidade, espalhabilidade, viscosidade, estabilidade (resistência a centrifugação) e teor alcoólico de 4 amostras (2 amostras industrializadas, denominadas A e B adquiridas em diferentes farmácias de manipulação da cidade, e 2 amostras magistrais, denominadas de amostra C e D. Sendo assim, observou-se que nenhuma das amostras se enquadraram nos parâmetros estabelecidos, como o pH mais ácido, densidade e viscosidade fora do padrão, diferentes comportamentos de espalhabilidade e teor alcoólico abaixo do ideal, apontando inconformidades que afetam a qualidade e ação do produto. Os resultados encontrados nesse estudo possibilitam concluir que as amostras de álcool gel de origem magistral apresentaram-se muito semelhante em termos de qualidade aos produtos industrializados. Portanto, entende-se que, apenas uma elaboração de leis não seja suficiente para garantir a qualidade e segurança do produto, se faz necessário uma fiscalização mais rigorosa e elaboração de leis mais qualificadas.

It is already known that hand hygiene is the main weapon in the prevention of infectious diseases inside and outside hospitals. In the case of the SARSCoV-2, hand hygiene is essential, in view of the possibility of contamination through direct contact with respiratory droplets or through indirect contact. There are several options of antiseptic products available on the market for use by the population. However, none are 100% effective in all situations. Among these different products available, 70% ethanol is the most used for application in the hands, being conveyed in the pharmaceutical form of a gel to facilitate the application. The pharmaceutical gel forms containing 70% ethanol can be industrialized or manipulated. When these formulations are manipulated, they are exempt from registration with the Health Surveillance Agency (ANVISA), not even requiring the safety and efficacy tests that are required for the registration of industrialized products. For manipulated products, only tests of description, appearance, organoleptic characteristics (color and odor), pH and weight are carried out. Thus, this work aimed to evaluate the quality, including physicochemical characteristics of alcohol gel samples handled in the city of Irecê-Ba, and compare them with an industrialized product of a known brand. The organoleptic aspects and characteristics, determination of the hydrogen potential (pH), density, spreadability, viscosity, stability (resistance to centrifugation) and alcohol content of 4 samples (2 industrialized samples, called A and B acquired in different compounding pharmacies) were analyzed of the city, and 2 magisterial samples, called sample C and D. Therefore, it was observed that none of the samples fit the established parameters, such as more acidic pH, non-standard density and viscosity, different spreadability behaviors and content alcohol below ideal, pointing out nonconformities that affect the quality and action of the product. The results found in this study make it possible to conclude that the samples of magistral alcohol gel were very similar in terms of quality to the industrialized products. Therefore, it is understood that just drafting laws is not enough to guarantee the quality and safety nce of the product, more rigorous inspection and the elaboration of more qualified laws are necessary.

Ya se sabe que la higiene de las manos es la principal arma en la prevención de enfermedades infecciosas dentro y fuera de los hospitales. En el caso del SARSCoV- 2, la higiene de las manos es esencial, ante la posibilidad de contaminación por contacto directo con gotitas respiratorias o por contacto indirecto. Existen varias opciones de productos antisépticos disponibles en el mercado para uso de la población. Sin embargo, ninguno es eficaz al 100% en todas las situaciones. Entre estos diferentes productos disponibles, el etanol al 70% es el más utilizado para aplicación en las manos, siendo vehiculado en la forma farmacéutica de gel para facilitar la aplicación. Las formas farmacéuticas en gel que contienen 70% de etanol pueden ser industrializadas o manipuladas. Cuando estas formulaciones son manipuladas, están exentas de registro en la Agencia de Vigilancia Sanitaria (ANVISA), no exigiendo ni siquiera las pruebas de seguridad y eficacia que se exigen para el registro de productos industrializados. Para los productos manipulados, sólo se realizan pruebas de descripción, apariencia, características organolépticas (color y olor), pH y peso. Así, este trabajo tuvo como objetivo evaluar la calidad, incluyendo las características fisicoquímicas de muestras de alcohol gel manipuladas en la ciudad de Irecê-Ba, y compararlas con un producto industrializado de marca conocida. Se analizaron los aspectos y características organolépticas, determinación del potencial de hidrógeno (pH), densidad, untabilidad, viscosidad, estabilidad (resistencia a la centrifugación) y grado alcohólico de 4 muestras (2 muestras industrializadas, denominadas A y B adquiridas en diferentes farmacias de composición) de la ciudad, y 2 muestras magistrales, denominadas muestra C y D. Así, se observó que ninguna de las muestras se ajustaba a los parámetros establecidos, tales como pH más ácido, densidad y viscosidad no estándar, diferentes comportamientos de untabilidad y contenido alcohólico por debajo del ideal, señalando no conformidades que afectan a la calidad y acción del producto. Los resultados encontrados en este estudio permiten concluir que las muestras de alcohol magistral en gel fueron muy similares en términos de calidad a los productos industrializados. Por lo tanto, se entiende que la mera elaboración de leyes no es suficiente para garantizar la calidad y seguridad nce del producto, siendo necesaria una inspección más rigurosa y la elaboración de leyes más cualificadas.

Structural investigation of anti-Trypanosoma cruzi 2-iminothiazolidin-4-ones allows the identification of agents with efficacy in infected mice.

We modified the thiazolidinic ring at positions N3, C4, and C5, yielding compounds 6-24. Compounds with a phenyl at position N3, 15-19, 22-24, exhibited better inhibitory properties for cruzain and against the parasite than 2-iminothiazolidin-4-one 5. We were able to identify one high-efficacy trypanocidal compound, 2-minothiazolidin-4-one 18, which inhibited the activity of cruzain and the proliferation of epimastigotes and was cidal for trypomastigotes but was not toxic for splenocytes. Having located some of the structural determinants of the trypanocidal properties, we subsequently wished to determine if the exchange of the thiazolidine for a thiazole ring leaves the functional properties unaffected. We therefore tested thiazoles 26-45 and observed that they did not inhibit cruzain, but they exhibited trypanocidal effects. Parasite development was severely impaired when treated with 18, thus reinforcing the notion that this class of heterocycles can lead to useful cidal agents for Chagas disease.

Alternativas terapêuticas no combate à Esquistossomose Mansônica / Alternative therapeutic agents to combat Manson´s schistosomiasis

A esquistossomose mansônica é classificada pelo Ministério da Saúde como uma doença negligenciada, causada pelo trematódeo intravascular Schistosoma mansoni. As precárias condições de higiene estão diretamente relacionadas às áreas endêmicas, bem como à pobreza e ao baixo desenvolvimento econômico. Na atualidade, o praziquantel é o fármaco de escolha utilizado para o tratamento dessa patologia. No entanto, o mesmo é relativamente tóxico devido à sua baixa solubilidade, além de relatos acerca de parasitas resistentes ao tratamento. Nesse contexto, faz-se necessário buscar novas alternativas terapêuticas que possam ser utilizadas no tratamento dessa doença. Esta revisão trata da busca por uma nova quimioterapia e sugere a possibilidade de que formas mais adequadas de vetorização de medicamentos já existentes sejam capazes de associar vantagens terapêuticas ao fármaco de escolha para o tratamento proposto, de forma que a população infectada receba seus benefícios.

Manson´s schistosomiasis is classified by the Ministry of Health as a neglected disease caused by the intravascular trematode Schistosoma mansoni. Endemic areas are directly related to poor hygienic conditions, as well as poverty and a low level of economic development. Currently, praziquantel is the drug of choice used to treat this condition, but it is relatively toxic, due to its low solubility, and there are reports of the parasite developing resistance to the treatment. In this context, there is a need to search for new therapeutic agents that can be used to treat this disease. This review covers the search for a new chemotherapy and suggests the possibility that the best existing drug vectorization systems may be able to combine therapeutic advantages with the drug of choice for the treatment, to the benefit of the infected population.