Development of metformin HCl granules using brown flaxseed mucilage as a retardant polymer: effects of polymer and drug ratio

Abstract Flaxseed (Linum usitatissimum L.) is the seed of a multipurpose plant of pharmaceutical interest, as its mucilage can be used as a natural matrix to develop extended-release dosage forms and potentially replace synthetic polymers. In this study, a 3² factorial design with two replicates of the central point was applied to optimize the development of extended-release granules of metformin HCl. The total fiber content of the mucilage as well as the friability and dissolution of the formulations were evaluated. The lyophilized mucilage presented a high total fiber content (42.63%), which suggests a high efficiency extraction process. Higher concentrations of the mucilage and metformin HCl yielded less friable granules. In addition, lower concentrations of metformin HCl and higher concentrations of the mucilage resulted in slower drug release during the dissolution assays. The release kinetics for most formulations were better represented by the Hixson-Crowell model, while formulations containing a higher concentration of the mucilage were represented by the Korsmeyer-Peppas model. Nonetheless, five formulations showed a longer release than the reference HPMC formulation. More desirable results were obtained with a higher concentration of the mucilage (13-18%) and a lower concentration of metformin (40%).

Eugenia sulcata (Myrtaceae) Nanoemulsion Enhances the Inhibitory Activity of the Essential Oil on P2X7R and Inflammatory Response In Vivo.

P2X7R is a purinergic receptor with broad expression throughout the body, especially in immune system cells. P2X7R activation causes inflammatory mediators to release, including interleukin-1ß (IL-1ß), the processing and release of which are critically dependent on this ion channel activation. P2X7R's therapeutic potential augments the discovery of new antagonistic compounds. Thus, we investigated whether the Eugenia sulcata essential oil could block P2X7R activity. The essential oil (ESO) dose-dependently inhibited ATP-promoted PI uptake and IL-1ß release with an IC50 of 113.3 ± 3.7 ng/mL and 274 ± 91 ng/mL, respectively, and the essential oil nanoemulsion (ESON) improved the ESO inhibitory effect with an IC50 of 81.4 ± 7.2 ng/mL and 62 ± 2 ng/mL, respectively. ESO and ESON reversed the carrageenan-activated peritonitis in mice, and ESON exhibited an efficacy higher than ESO. The majority substance from essential oil, ß-caryophyllene, impaired the ATP-evoked PI uptake and IL-1ß release with an IC50 value of 26 ± 0.007 ng/mL and 97 ± 0.012 ng/mL, respectively. Additionally, ß-caryophyllene reduced carrageenan-induced peritonitis, and the molecular modeling and computational simulation predicted the intermolecular interactions in the P2X7R situs. In silico, results indicated ß-caryophyllene as a potent allosteric P2X7R antagonist, although this substance may present toxic effects for humans. These data confirm the nanoemulsion of essential oil from E. sulcata as a promisor biotechnology strategy for impaired P2X7R functions and the inflammatory response.

Risk assessment of coffees of different qualities and degrees of roasting.

During the coffee beans roasting process, occurs the formation of polycyclic aromatic hydrocarbons, which are associated with the incidence of cancer in humans. This study aimed to evaluate the influence of coffee bean quality and roasting degree regarding mutagenicity, cytotoxicity and genotoxicity. Six samples of coffee drink made with roasted and ground Coffea arabica beans from different qualities and roast degrees were used after freeze-drying. Both commercial and special quality grains suffered light, medium and dark roasting. According to the Salmonella/microsome assay, the highest concentration of commercial grain sample (dark roast) significantly increased the number of revertants of the TA98 strain in the absence of metabolization. All the samples induced cytotoxicity to HepG2 cells. These effects can be ranked in the following order from most to least toxic: medium roast - special grain > light roast - special grain > dark roast - commercial grain > dark roast - special grain > light roast - commercial grain > medium roast - commercial grain. None of the samples induced genotoxicity in HepG2 cells. Our findings show that the harmful effects of coffee depend not only on the degree of roasting but also on the grain quality.

Foam mat drying of Tommy Atkins mango: Effects of air temperature and concentrations of soy lecithin and carboxymethylcellulose on phenolic composition, mangiferin, and antioxidant capacity.

In this study, foam mat drying was applied to Tommy Atkins mango. Using a multifactorial design, the effect of soy lecithin (L) and carboxymethylcellulose (CMC) used as foam stabilizers (0-1.50g/100g), as well as temperature (T) (53-87°C), on phenolic content and antioxidant capacity of mango were evaluated. Mango pulp contains antioxidant, such as mangiferin, that can be utilized in foods to enhance their functional properties. Our results indicated that L and T had negative effects (p<0.05) on the phenolic content and antioxidant capacity, whereas CMC had a positive effect (p<0.05). Increasing the total amount of phenolic compounds present in dried mango contributed to the higher antioxidant capacity after the drying process. This study concluded that a drying T of 80°C, and a concentration of 0.30g/100g of CMC and L are optimal for increased retention of phenolic compounds and antioxidant capacity.