Immunomodulatory and Anticancer Effects of Fridericia chica Extract-Loaded Nanocapsules in Myeloid Leukemia.

Nanocapsules provide selective delivery and increase the bioavailability of bioactive compounds. In this study, we examined the anticancer and immunomodulatory potential of Fridericia chica (crajiru) extract encapsulated in nanocapsules targeting myeloid leukemias. Nanocapsules containing crajiru (nanocapsules-CRJ) were prepared via interfacial polymer deposition and solvent displacement. Size and polydispersity were measured by dynamic light scattering. Biological assays were performed on leukemia cell lines HL60 and K562 and on non-cancerous Vero cells and human PBMC. The anticancer activity was evaluated using cytotoxicity and clonogenic assays, while the immunomodulatory activity was evaluated by measuring the levels of pro- and anti-inflammatory cytokines in PBMC supernatants treated with concentrations of nanocapsules-CRJ. Nanocapsules-CRJ exhibited significant cytotoxic activity against HL60 and K562 cells at concentrations ranging from 0.75 to 50 µg/mL, with the greatest reductions in cell viability observed at 50 µg/mL (p < 0.001 for HL60; p < 0.01 for K562), while not affecting non-cancerous Vero cells and human PBMCs. At concentrations of 25 µg/mL and 50 µg/mL, nanocapsules-CRJ reduced the formation of HL60 and K562 colonies by more than 90% (p < 0.0001). Additionally, at a concentration of 12 µg/mL, nanocapsules-CRJ induced the production of the cytokines IL-6 (p = 0.0002), IL-10 (p = 0.0005), IL-12 (p = 0.001), and TNF-α (p = 0.005), indicating their immunomodulatory potential. These findings suggest that nanocapsules-CRJ hold promise as a potential therapeutic agent with both cytotoxic and immunomodulatory properties.

Encapsulation of camu-camu extracts using prebiotic biopolymers: Controlled release of bioactive compounds and effect on their physicochemical and thermal properties.

Camu-camu (Myrciaria dubia [H.B.K] McVaugh) is a Amazonian fruit rich in ascorbic acid and phenolic compounds, and has been attracting great interest from the food, pharmaceutical and nutraceutical industries due to its potential health benefits. The bioactive compounds from camu-camu are considered sensitive and unstable, resulting in nutritional losses and impairment of its commercialization and export. For this reason, the camu-camu extract (pulp and peel) was subjected to microencapsulation by spray drying process using maltodextrin (MD), inulin (IN), and oligofructose (OL) as carrier agents. Lyophilized in natura camu-camu extract (CEL) was also evaluated. Thus, physicochemical and thermal properties and controlled release at different temperatures (25 °C and 35 °C) were investigated. In contrast with the IN and OL microparticles, the MD microparticles showed lower density and hygroscopicity, besides greater thermal stability, antioxidant activity, and retention of ascorbic acid and anthocyanins. FTIR spectra allowed the qualitative evidence of encapsulation of the bioactive compounds from the camu-camu extract. The highest percentage of volatile compounds was observed in IN microparticles, followed by OL and MD microparticles. The major group of compounds identified in CEL were terpenes (88%). The Korsmeyer-Peppas mathematical model allowed to describe the controlled release behavior of ascorbic acid and anthocyanins in the powder extracts. The controlled release followed a Fickian diffusion mechanism (n ≤ 0.43). The increase of temperature from 25 °C to 35 °C influenced on the release of bioactive compounds in all treatments, showing greater release for MD microparticles. The encapsulating materials were considered effective for the production of camu-camu extract powder, contributing to the better use of this Amazonian fruit. In addition, the encapsulation process increased the stability of its bioactive compounds, representing a tool to facilitate their incorporation in several matrices to act as antioxidant and coloring agents, as well as nutraceutical.

Eudragit E as excipient for production of granules and tablets from Phyllanthus niruri L spray-dried extract.

The aim of this study was to investigate the feasibility of using Eudragit E as a granulating agent for a spray-dried extract from Phyllanthus niruri to obtain tablets containing a high dose of this product. The granules were developed by wet granulation and contained 2.5%, 5.0%, and 10.0% Eudragit E in the final product concentration. The tablets were produced on a single-punch tablet press by direct compression of granules using 0.5% magnesium stearate as a lubricant. The tablets were elaborated following a 2 x 3 factorial design, where Eudragit E concentration and compression force were the independent variables, and tensile strength and the extract release of the tablets were the dependent variables. All granules showed better technological properties than the spray-dried extract, including less moisture sorption. The characteristics of the granules were directly dependent on the proportion of Eudragit E in the formulation. In general, all tablets showed high mechanical resistance with less than 1% friability, less moisture sorption, and a slower extract release profile. The Eudragit E concentration and compression force of the tablets significantly influenced both dependent variables studied. In conclusion, Eudragit E was efficient as a granulating agent for the spray-dried extract, but additional studies are needed to further optimize the formulations in order to achieve less water sorption and improve the release of the extract from the tablets.

Spray dried extract of Calophyllum brasiliense Cambés produces a potent hypoglycemic effect and improves total serum cholesterol and triglycerides in diabetic rats / El extracto secado por pulverización de Calophyllum brasiliense cambés produce un potente efecto hipoglucémico y mejora el colesterol sérico total y los triglicéridos en ratas diabéticas / O extrato seco por aspersão de Calophyllum brasiliense Cambés produz um potente efeito hipoglicemiante e melhora o colesterol total e triglicérideos em ratos diabéticos

SUMMARY Introduction: The species Calophyllum brasiliense Cambés (Calophyllaceae) is widespread throughout Central and South America. The stem bark infusion is used for lowering blood glucose. Aim: To optimize the spray dry extract ofthis plant using a D-optimal experimental design. Materials and methods: As factors were used the air-drying speed (3.5-4.5 m3/h), the feed flow rate of the suspension (5-11 mL/ min), and the inlet air temperature (90-130 °C). The dried extract was characterized by measuring the phenolics and flavonoids content, moisture, the water activity, apparent densities, flowability, and compressibility. The antioxidant activity, the inhibitory activity of lipase and alpha-glycosidase, and the antiglycant activity of the spray dried extract (SDE) were evaluated. Subsequently, the hypoglycemic activity was evaluated in rats by monitoring the blood glucose level, triglycerides, and cholesterol. Results: Inlet air temperature and feed flow rate were the factors that most affected the yield and phenolic content. SDE showed a potent antioxidant effect (IC50 1.83 μg/mL), a potent a-glycosidase (IC50 74.45 μg/mL) and pancreatic lipase (IC50 27.33 μg/mL) inhibition. A potent antiglycation effect (IC50 9.45^g/mL) was also observed. Conclusion: the SDE showed a potent hypoglycemic effect at 100 mg/kg. These results suggest that SDE could activate four important pathways that can contribute to diabetes control.

Resumen Introducción: la especie Calophyllum brasiliense (Calophyllaceae) está muy extendida en Centro y Suramérica. La infusión del tronco reduce los niveles de glucosa en sangre. bjetivo: optimizar el extracto seco por aspersión (SDE) de esta planta utilizando un diseño experimental D-óptimal. Materiales y métodos: como factores se utilizaron la velocidad del gas secante (aire, 3,5-4,5 m3/h), la temperatura de entrada del aire fue 90-130 °C y la velocidad de alimentación, 5-11 mL/min. Se determinó el contenido de fenoles y flavonoides en el extracto seco, la humedad residual, la actividad del agua, las densidades aparentes, fluidez y compresibilidad. Se evaluó la actividad antioxidante e inhibidora de lipasa y alfa-glicosidasa y la actividad antiglicante. También se evaluó la actividad hipoglicemiante midiendo glucosa en sangre, triglicéridos y colesterol. Resultados: la temperatura del aire de entrada y la velocidad de alimentación afectaron, significativamente, el rendimiento y contenido de fenoles. El SDE mostró un potente efecto antioxidante (IC50 1,83 μg/mL), una potente inhibición de a-glicosidasa (IC50 74,45 μg/mL) y de lipasa pancreática (IC50 27,33 μg/ mL). Se observó un fuerte efecto antiglicante (IC50 9,45 μg/mL). Conclusiones: el SDE mostró un potente efecto hipoglicemiante a 100 mg/kg. Estos resultados sugieren que el SDE podría actuar activando cuatro vías importantes para el control de la diabetes.

RESUMO Introdução: a espécie Calophyllum brasiliense (Calophyllaceae) é amplamente distribuída na América do Sul e Central. A infusão da casca do caule reduz os níveis de glicose no sangue. Objetivo: otimizar o extrato seco por pulverização (SDE) desta planta usando um planejamento experimental D-ótimo. Materiais e métodos: a velocidade do gás de secagem ar (3,5-4,5 m3/h), a temperatura de entrada do ar (90-130 °C) e a taxa de alimentação (5-11 mL/min) foram usados como fatores. Foi determinado o teor de fenóis e flavonóides no extrato seco, a umidade residual, a atividade de água, as densidades aparentes, a fluidez e a compressibilidade. Avaliou-se a atividade antioxidante e a atividade inibitória de lipase e alfa-glicosidase, e a atividade antiglicante do extrato seco. A atividade hipoglicêmica foi avaliada em ratos diabeticos, medindo a glicose no sangue, triglicerídeos e colesterol. Resultados: a temperatura de entrada do ar e a taxa de alimentação afetaram significativamente o desempenho e o conteúdo de fenois. O SDE mostrou um potente efeito antioxidante (IC50 1,83 μg/mL), uma significativa inibição de a-glicosidase (IC50 74,45 ig/mL) e da lipase pancreática (IC50 27,33 μg/mL). Um forte efeito antiglicante também foi observado (IC50 9,45 μg/mL). O SDE mostrou um forte efeito hipogli-cemiente à concentração de 100 mg/kg. Conclusões: Esses resultados sugerem que o SDE poderia atuar ativando quatro vias importantes para o controle do diabetes.

Extract from Eugenia punicifolia is an antioxidant and inhibits enzymes related to metabolic syndrome.

The present study aimed to investigate in vitro biological activities of extract of Eugenia punicifolia leaves (EEP), emphasizing the inhibitory activity of enzymes related to metabolic syndrome and its antioxidant effects. The antioxidant activity was analyzed by free radicals scavengers in vitro assays: DPPH·, ABTS(·+), O2(·−), and NO· and a cell-based assay. EEP were tested in inhibitory colorimetric assays using α-amylase, α-glucosidase, xanthine oxidase, and pancreatic lipase enzymes. The EEP exhibited activity in ABTS(·+), DPPH·, and O2(·−) scavenger (IC50 = 10.5 ± 1.2, 28.84 ± 0.54, and 38.12 ± 2.6 µg/mL), respectively. EEP did not show cytotoxic effects, and it showed antioxidant activity in cells in a concentration-dependent manner. EEP exhibited inhibition of α-amylase, α-glucosidase, and xanthine oxidase activities in vitro assays (IC50 = 122.8 ± 6.3; 2.9 ± 0.1; 23.5 ± 2.6), respectively; however, EEP did not inhibit the lipase activity. The findings supported that extract of E. punicifolia leaves is a natural antioxidant and inhibitor of enzymes, such as α-amylase, α-glucosidase, and xanthine oxidase, which can result in a reduction in the carbohydrate absorption rate and decrease of risks factors of cardiovascular disease, thereby providing a novel dietary opportunity for the prevention of metabolic syndrome.

Avaliaçao da viabilidade de compressao direta de formulaçoes contendo alto teor de produto seco nebulizado de maytenus ilicifolia / Direct compression feasibility of formulations containing high amount of maytenus ilicifolia spray dried extract

O objetivo deste trabalho foi availar a viabilidade de compressao direta de formulaçoes contendo alto dosagem de produto seco nebulizado de maytenus ilicifolia e, através de um planejamento fatorial 2(3), a influência de adjuvantees farmacêuticos sobre as caracteristicas mecânicas do produto compactado. Os fatores estudiados foram tipo de desagregante (croscarmelose sódica e glicolato de amido sódico), lubrificante (estearato de magnesio e dióxido de silício coloidal) e material de carga/aglutinante (celulose microcristalina e lactose). Foram analizados os parâmetros de compactaçao das formulaçoes e as características mecânicas dos produtos compactados. O efeito mas intenso sobre a friabilidade e o tempo de desintegraçao dos compacto foi causado pelo tipo de material de carga/aglutinante, embora con menor intensidade os demais adjuvantes tembén apresentaram efeito significativo sobre as variáveis estudadas