Nanotechnology in pharmaceutics has the potential to improve drug efficacy by influencing drug distribution in tissues. Nanocarriers have been developed as drug delivery systems to be administered by different biological routes. To ensure the nanotechnological properties, pre-formulation studies are especially critical in determining the influence of the process parameters on the size and polydispersity of particles. Thus, the objective of this work was to establish the mechanism of self-assembly, by determining the influence of the critical aggregation concentration of the materials in the organic phase on the final average particle size and polydispersity of polymeric lipid-core nanocapsules obtained by interfacial deposition of polymer. Measurements of the surface tension and viscosity of the organic and aqueous phases were correlated with the particle size and the concentration of raw materials. We demonstrated that the lipid-core nanocapsules are formed on the nanoscopic scale as unimodal distributions, if the aggregation state of raw materials in the organic phase tends to infinite dilution. The strategy for controlling the particle size distribution is a valuable tool in producing lipid-core nanocapsule formulations with different loading capacities intended for therapeutics.

Nine Brazilian Amaryllidaceae species were studied for their alkaloid composition and acetylcholinesterase (AChE) inhibitory activity via GC-MS and a modified Ellman assay, respectively. A total of thirty-six alkaloids were identified in these plants, of which Hippeastrum papilio and H. glaucescens exhibited the highest galanthamine content and the best IC 50 values against AChE. Furthermore, Hippeastrum vittatum and Rhodophiala bifida also showed notable AChE inhibitory effects. X-ray crystallographic data for four galanthamine-type compounds revealed significant differences in the orientation of the N-methyl group, which are shown to be related to AChE inhibition.

Objective: To investigate the extent to which exercise is associated with symptoms in patients with severe obstructive sleep apnea (OSA). Methods: We included subjects with an apnea-hypopnea index (AHI) > 30 events/h who completed validated sleep and exercise questionnaires. We compared symptom frequency/scores between exercisers and nonexercisers, adjusting for the usual confounders. Results: The sample included 907 nonexercisers and 488 exercisers (mean age, 49 ± 14 years; mean AHI, 53 ± 20 events/h; 81% men). Nonexercisers and exercisers differed significantly in terms of obesity (72% vs. 54%), the mean proportion of sleep in non-rapid eye movement stage 3 sleep (9 ± 8% vs. 11 ± 6%), and tiredness (78% vs. 68%). Nonexercisers had a higher symptom frequency/scores and poorer sleep quality. Adjustment for exercise weakened the associations between individual symptoms and the AHI, indicating that exercise has a mitigating effect. In binary logistic models, exercise was associated with approximately 30% lower adjusted questionnaire1 score > 2, tiredness; poor-quality sleep, unrefreshing sleep, and negative mood on awakening. Although the odds of an Epworth Sleepiness Scale score > 10 were lower in exercisers, that association did not withstand adjustment for confounders. Conclusions: Exercise is associated with lower frequency/intensity of symptoms in patients with severe OSA. Because up to one third of patients with severe OSA might exercise regularly and therefore be mildly symptomatic, it is important not to rule out a diagnosis of OSA in such patients.

In nanomedicine, different nanomaterials and nanoparticles have been proposed as therapeutic agents or adjuvants, as well as diagnosis devices. Considering that the principal cause of the ulcerations is the imbalance among the gastric juice secretion and the protection provided by the mucosal barrier and the neutralization of the gastric acid, as well as that nanoparticles are able to accumulate in the gastro-intestinal tissues, we proposed a 2(2) factorial design to evaluate the influence of the chemical composition and the volume fraction of the dispersed phase on the gastric protective effect against ulceration induced by ethanol. Cocoa-theospheres (CT) and lipid-core nanocapsules (LNC) (two different kinds of surfaces: lipid and polymeric, respectively) prepared at two different concentrations of soft materials: 4% and 12% (w/v) were produced by high pressure homogenization and solvent displacement methods, respectively. Laser diffraction showed volume-weighted mean diameters ranging from 133 to 207 nm, number median diameters lower than 100 nm and specific surfaces between 41.2 and 51.2 m(2) g(-1). The formulations had pH ranging from 4.7 to 6.3; and zeta potential close to -9 mV due to their coating with polysorbate 80. The ulcer indexes were 0.40 (LNC(4)) and 0.48 (CT(4)) for the lower total administered areas (3.3 and 4.1 m(2)g(-1), respectively), and 0.09 (LNC(12) and CT(12)) for the higher administered areas (10.0 and 12.0 m(2) g(-1), respectively). LNC(4), LNC(12) and CT(12) showed lower levels in the lipid peroxidation assay when compared either to the negative control (saline) or to CT(4). LNC(12) and CT(12) showed similar TBARS levels, as well as CT(4) was similar to the negative control. SEM analysis of the stomach mucosa showed coatings more homogenous and cohesive when LNC formulations were administered compared to the correspondent CT formulations. The higher total area of administered nanoparticles showed film formation. Moreover, LNC(12) provided a more thick and cohesive film, completely covering the mucosal surface. In conclusion, both kinds of formulations are able to prevent ulceration induced by ethanol in rats. The 2(2) factorial design showed that the chemical composition had a strong influence when the lower areas of nanoparticles are administered, while when the higher areas are used this is the more influencing parameter on the gastroprotection.

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Introduction: Caffeinated drinks are used for improve performance. Animal models represent investigational strategy that circumvents most of the drawbacks of research in humans, including motivational factors and the placebo effect. No animal model that could test whether different forms of administering caffeine affect exercise propensity was found in the literature.

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