Spray-drying of casein/pectin bioconjugate microcapsules containing grape (Vitis labrusca) by-product extract.

Novel microcapsules containing grape peel by-product extract were obtained. In this pursuit, complex coacervation of casein/pectin bioconjugate and spray-drying were combined. We have investigated the role of the dispersion feed rate (FR), drying air inlet temperature (IT) and drying air flow rate (AR) in the drying yield, microencapsulation efficiency, total polyphenols and anthocyanins contents, antioxidant activity, and morphology of the products. Also, the first-order degradation kinetics of the phytochemicals for both the extract and dried microcapsules was assessed and compared. The loss on the phytochemicals during spray-drying was attenuated in up to 88%, and the IT was the main factor affecting the particle properties. The polyphenols on the extract interacted with the polymers, influencing the assemble of the bioconjugate and the particle's features. Such microencapsulation strategy enhanced the thermal stability of the phytochemicals and rendered biocompatible and biodegradable products of which the nutraceutical and cosmeceutical application may have potential.

Protective effects of quercetin-loaded microcapsules on the enteric nervous system of diabetic rats.

Quercetin-loaded microcapsules (QLM) promote controlled release and higher bioavailability of quercetin, an antioxidant and neuroprotective agent. We evaluated the antioxidant effect of QLM on enteric innervation and in the oxidative status of the ileum of diabetic rats. Wistar adult rats (Rattus norvegicus) were used in six groups containing normoglycemic (N), diabetic (D) and either normoglycemic or diabetic groups treated with QLM at a dose of 10 mg/kg (NQ10 and DQ10, respectively) or 100 mg/kg (NQ100 and DQ100, respectively). DQ10 e DQ100 did not prevent overall neuronal loss in the total and cholinergic populations. Nitrergic population showed differences regarding the treatments: DQ10 preserved neurons in the nitrergic population whilst DQ100 increased nitrergic loss. Evaluation of the redox status showed pro-oxidant effects in NQ100 by t-butyl-induced chemiluminescence analysis. We observed a reduction in the carbonylic content and an increase of low molecular weight antioxidants for DQ10 e DQ100. Therefore, QLM treatment at a dose of 10 mg/kg acted positively on nitrergic neurons reducing oxidative damage induced by diabetes.

Prevention of UVB radiation-induced oxidative stress in mice by topical administration of Azadirachta indica(neem) extract

Neem tree (Azadirachta indica A. Juss. fam. Meliaceae) has been extensively employed to combat diverse pathologies. Moreover, it has been described that its leaf extract present anticarcinogenic action. Thus, the neem extract (NE) chemical and antioxidant properties was evaluated, and also, the capacity of two dermatological formulations incorporated with neem extract (F1 and F2) to avoid oxidative UVB-induced skin injury in hairless mice. NE constituents were investigated and free radical scavenging ability were determined by different methods in vitro. Skin from mice treated with F1 and F2 and submitted to UVB radiation were tested for different parameters of inflammation and oxidative injury. Results show that the NE polyphenol and flavonoid content were 135.30 and 37.12mg/g, respectively. High performance liquid chromatography (HPLC) results demonstrated the existence of azarachtin, rutin, ursolic acid and tannic acid. NE presented scavenging ability by ABTS radical, ferric-reducing antioxidant power (FRAP), inhibition of lipid peroxidation and iron chelation. In vivo, it was observed that mice treated with F1 and F2 showed amelioration of the inflammation by reducing UVB induced skin edema. However, only samples from animals treated with F1 had lower neutrophil recruitment (measured by myeloperoxidase activity), and returning the oxidative status to baseline levels in parameters such as reduced glutathione level, ferric reducing ability (FRAP), and scavenging of free radical (ABTS). Concluding, NE demonstrated a good antioxidant property in vitro, and the data suggest the use of NE added F1 to prevent skin damage caused by UVB irradiation.(AU)

Influência do armazenamento de suspensão bacteriana na respostainflamatória em camundongos / Influence of bacterial suspension storage in the inflammatory response in mice

O preparo de suspensão bacteriana é procedimento importante para avaliação da inflamação e podeser obtida por diferentes métodos que precisam ou não do passo de armazenamento. O objetivo destetrabalho foi investigar a influência do armazenamento de suspensão de Staphylococcus aureus na viabilidade bacteriana e sua influência na inflamação in vivo. A suspensão bacteriana de S. aureus ATCC 6538 foi preparada visualmente seguindo o grau 4 da Escala de McFarland. A viabilidade bacteriana nessa solução foi determinada pela contagem de UFC, a qual foi utilizada para induzir artrite séptica e peritonite. O armazenamento por 24 h reduziu as UFC de S. aureus. Essa redução da viabilidadebacteriana resultou em diminuição da hiperalgesia mecânica, edema e recrutamento leucocitário na artriteséptica, e recrutamento leucocitário e produção de citocinas na peritonite bacteriana. Estes resultadosdemonstraram que o armazenamento de suspensão bacteriana afetou sua viabilidade, resultando emdiminuição da resposta inflamatória in vivo, sugerindo a importância de padronizar procedimentos parao preparo de suspensão bacteriana. Uma abordagem concebível seria determinar o número de UFC em um específico grau da Escala de McFarland, o qual permitirá o preparo e o uso de uma suspensão bacteriana no mesmo dia para os testes in vivo.

The preparation of bacterial suspension is an important procedure used in laboratories for inflammatoryevaluation protocols and can be obtained by different methods that need or not need step storage. The aimof this work was investigate the influence of storage of Staphylococcus aureus suspension in bacterialviability and its influence in bacteria-induced inflammation in vivo. The bacterial suspension of S. aureus ATCC 6538 was prepared accordingly to 4th degree of McFarland’s Scale by visual comparison. This suspension was used to determine by CFU counting the bacterial viability and for administration to the animals to induce septic arthritis and peritonitis. Twenty four hours of storage reduced the S. aureus CFU. As a consequence of reduced bacterial viability, was detected reduced mechanical hyperalgesia, edema and leukocyte recruitment in septic arthritis and leukocyte recruitment and cytokine production bacterial peritonitis. These results demonstrate that storage of bacterial suspension affected bacterialviability, which resulted in diminished inflammatory response in vivo, raising the importance of standardprocedures for bacterial suspension preparation. A conceivable approach would be to determine the number of CFU at a specific McFarland’s scale degree, which will allow the preparation and use a bacterial suspension in the same day for in vivo testing.

The importance of coating standardization in gastro-resistant capsules produced in magistral pharmacy / Importância da padronização dos revestimentos utilizados em cápsulas gastrorresistentes produzidas em farmácia magistral

Gastro-resistant capsules are often used for several purposes, such as protection of unstable drugs in acid medium to the action of gastric fluids or protection of the gastric mucosa to irritants drugs. The aim of this study was to verify the variation of preparations of capsules coating with cellulose acetate phthalate and methacrylic acid copolymer, without drug addition, in 7-10% coating concentrations, prepared manually with four or five immersions in tested coating solution. Results were analyzed considering the formulation's disintegration test. Within the context of formulations under analysis, it was observed that the capsules coated with cellulose acetate phthalate 10% complied with the pharmacopeia's disintegration specifications. However, capsules coated with methacrylic acid copolymer did not show accordance with the pharmacopeia's specifications. The results emphasize the need for the standardization of coating methodology.

Cápsulas gastrorresistentes são frequentemente utilizadas com diversos propósitos, como a proteção de fármacos instáveis em meio ácido à ação dos fluidos gástricos ou proteção da mucosa gástrica à fármacos irritantes. O objetivo deste trabalho foi verificar a variação da preparação de revestimento de cápsulas com acetoftalato de celulose e copolímero do ácido metacrílico, sem adição de fármaco, em concentrações que variam de 7 a 10% de revestimento, preparadas manualmente com quatro a cinco camadas da solução dos revestimentos testados. Os resultados foram analisados considerando o teste de desintegração das formulações. Das formulações testadas, foi observado que as cápsulas revestidas com acetoftalato de celulose a 10% cumpriram com as especificações farmacopeicas quanto à desintegração. No entanto, cápsulas revestidas com copolímero de ácido metacrílico não mostraram conformidade com as especificações farmacopeicas. Os resultados obtidos enfatizam a necessidade de padronização da metodologia de revestimento.

Estudo comparativo de excipientes em diferentes técnicas de preparaçäo de comprimidos de cloridrato de propranolol / Comparative study of excipients for propanolol hydrochloryde tablets prepared by means of diferent techniques

A hipertensäo arterial sistêmica (HAS) é um dos mais importantes fatoresw de risco cardiovascular uma vez que contribui, mundialmente, com mais de 500 mil casos de acidentes cerebrovasculares (ACV), 150 mil mortes por hemorragia cerebral e aproximadamente um milhäo de infartos de miocárdio (IAM). No Brasil estima-se que cerca de 15 por cento dos indivíduos adultos possam ser rotulados como hipertensos. A hipertensäo pode ser prevenida com a mudança no estilo de vida, embora na maioria dos casos se faça necessário o tratamento farmacológico. O cloridrato de propranolol é o fármaco de escolha para hipertensos idosos que tiveram infarto prévio do miocárdio. Os comprimidos podem ser preparados por tres técnicas de fabricaçäo diferentes. A técnica de granulaçäo úmida é a mais comumente utilizada. Com o avanço de novos excipientes disponíveis no mercado para as indústrias farmacêuticas, tornou-se possível o emprego de técnica mais simples e econômica, melhorando a estabilidade física e química do produto, atingindo o objetivo de obter medicamentos eficazes e seguro. O objetivo deste trabalho foi desenvolver formulaçöes de cloridrato de propranolol variando-se os excipientes e técnicas de fabricaçäo. Os mesmos foram armazenados em estufa a 37 e 50§C com 90 por cento UR durante 90 dias e analisados em intervalos de tempo preestabelecidos. As formulaçöes foram avaliadas em funçäo dos aspectos físico e físico-químico