Stem bark extract of Poincianella pluviosa incorporated in polymer film: Evaluation of wound healing and anti-staphylococcal activities.

Poincianella pluviosa has already been described as capable of healing skin wounds. In an attempt to prolong contact of the drug with the wound, it was proposed in this study to evaluate wound healing using a crude extract (CE) of P. pluviosa incorporated in carboxymethylcellulose polymer films. The chromatographic profile of the semipurified fraction of P. pluviosa was evaluated by ultra-high performance liquid chromatography (UHPLC), confirming the compounds gallic acid, geraniin, and ellagic acid. The films were evaluated for their physical and mechanical properties, water vapor permeability, moisture absorption capacity, and FTIR spectroscopy. For in vivo experiments, wounds were made on the back of rats and treated daily for 4, 7, 10, or 14 days with film containing CE or control film. At the end of each period, skin permeation analysis and histological analysis were made using re-epithelialisation, cell proliferation, and collagen formation. Statistical significance was determined by GraphPad Prism using t test and Mann-Whitney test. Anti-staphylococcal activity was evaluated with standard strains of Staphylococcus aureus, methicillin-resistant, and coagulase negative. It was demonstrated that the presence of CE in the films increased the capacity to absorb water and decreased resistance and permeability. The CE of the film permeated the skin, reaching the dermis and was able to influence re-epithelisation, cell proliferation, and collagen formation. Satisfactory results were observed against S. aureus strains, particularly coagulase negative. Films with CE of P. pluviosa can be an alternative in the wound healing, protecting against opportunistic infections and giving comfort to the patient.

Chemical analysis of the semipurified extract of Paullinia cupana and evaluation of in vitro inhibitory effects against Helicobacter pylori.

Paullinia cupana Kunth, commonly known as guarana, is a native Brazilian plant species from the Amazon area that presents various biological effects, including antimicrobial action. The aim of this study was to chemically analyse the semipurified aqueous extract (AqF) of the plant and to evaluate the activity of crude (CE), ethyl-acetate (EAF), and AqF extracts against Helicobacter pylori. The chemical profile of AqF was determined based on solid analysis 13C-NMR, direct infusion mass spectrometry (ESI-MS), and MALDI-TOF. The 13C-NMR spectrum showed characteristics of flavan-3-ol and oligomeric proanthocyanidins. ESI-MS revealed the presence of procyanidin, caffeic acid and its derivatives. MALDI-TOF analysis detected procyanidins of up to 6 units and profisetinidins of up to 5 units. Whereas CE and EAF showed inhibitory activity against H. pylori, CE, EAF, and AqF presented not high inhibitory activity against urease. The results demonstrate the potential of P. cupana to control and prevent H. pylori infection.

Estudo de formulação de microesferas de acetobutirato de celulose com diferentes concentrações de Poloxamer 188 / Formulation study of cellulose acetate butyrate microspheres withdifferent concentrations of Poloxamer 188

Microesferas de liberação prolongada de diclofenaco de sódio (DFS) foram preparadas empregando o acetobutirato de celulose (ABC) para obtenção da matriz polimérica. Buscando modular a velocidade de liberação do fármaco, a adição de Poloxamer 188 na formulação foi testada, com diferentes proporções de ABC: Pluronic F68 (1:0; 9:1; 3:1 e 1:1). Com exceção da formulação contendo ABC e Pluronic F68 na proporção de 1:1, as outras formulações testadas conduziram à formação de partículas esféricas de tamanho micrométrico. Quando a misturaA BC: Pluronic F68 (1:1) foi empregada, ocorreu à precipitação de uma massa polimérica, sendo este efeito relacionado à elevada concentração do polímero hidrofílico na preparação. Quando comparado com as microesferas preparadas unicamente com ABC, o teor e a eficiência de encapsulação aumentaram com o acréscimo de Poloxamer 188 às formulações. Efeito semelhante foi observado na avaliação da velocidade de liberação do fármaco em meio tampão fosfato pH 7,5. Enquanto as microesferas preparadas apenas com ABC conduziram à liberação de 25% do fármaco encapsulado após 12 horas de ensaio, as microesferas preparadas com relação ABC:Pluronic 9:1 e 3:1 conduziram à liberação de 30% e 70% do fármaco, respectivamente.

Extended-release microspheres containing sodium diclofenac were prepared using the cellulose acetate butyrate (CAB) to obtain the polymer matrix. Looking modulate the rate of drug release, the addition of Poloxamer 188 at different concentrations into formulations was tested in order to obtain CAB to Poloxamer ratio of 1:0, 9:1, 3:1 and 1:1. Excepting for the formulation containing CAB and Poloxamer 1:1, the other formulations resulted in formation of spherical particles of micrometer size range. When the mixture CAB:Poloxamer (1:1) was employed, the precipitation of a polymeric mass occorred, and this effect was related to the high concentration of the hydrophilic polymer in the preparation. When compared to the microspheres prepared only with CAB, the drug content and the encapsulation efficiency increased with the addition of Poloxamer 188 in the formulations. A similar effect was observed in the evaluation of the rate of drug release in pH 7.5 phosphate buffer. While the microspheres prepared with CAB led to release of 25% of the encapsulated drug after 12 hours of testing, the microspheres prepared with CAB: Poloxamer 9:1 and 3:1 resulted in release of 30% and 70% of the drug, respectively.

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.