Composition influence on pulmonary delivery of rifampicin liposomes

The effects of lipid concentration and composition on the physicochemical properties, aerosol performance and in vitro toxicity activity of several rifampicin-loaded liposomes were investigated. To this purpose, six liposome formulations containing different amounts of soy phosphatidylcholine and hydrogenated soy phosphatidylcholine, with and without cholesterol and oleic acid, were prepared and fully characterized. Uni- or oligo-lamellar, small (~100 nm), negatively charged (~60 mV) vesicles were obtained. Lipid composition affected aerosol delivery features of liposomal rifampicin; in particular, the highest phospholipid concentration led to a better packing of the vesicular bilayers with a consequent higher nebulization stability. The retention of drug in nebulized vesicles (NER%) was higher for oleic acid containing vesicles (55% ± 1.4%) than for the other samples (~47%). A549 cells were used to evaluate intracellular drug uptake and in vitro toxicity activity of rifampicin-loaded liposomes in comparison with the free drug. Cell toxicity was more evident when oleic acid containing liposomes were used

Germination and Fermentation of Soybeans: Two Healthy Steps to Release Angiotensin Converting Enzyme Inhibitory Activity Compounds

Background and objective: Soybean is one of the most important grains with high proteins, good quality edible oils, appreciable amount of minerals and vitamins. Due to some disadvantages soybeans’ compounds affecting the flavor, odor and stability, different types and levels of processing are considered to make better products with healthy properties. Hypertension (high blood pressure) is one of the modern world diseases, which increases the risk of serious human health problems. There are several systems in humans’ body e.g. angiotensin converting enzyme regulator to blood pressure control. The aim of the present review is to report the effect of germination and fermentation on the concentration of bioactive compounds with angiotensin converting enzyme inhibitory properties. Results and conclusion: Many scientific research has demonstrated that germination (sprouting, also known as malting) and fermentation are two effective and inexpensive technologies improving soybean quality. During these two processes, anti-nutritional and bioactive compounds affecting human health e.g. anti-hypertension components have been removed and released, respectively. Furthermore, studies have shown effect of soybean isolated compounds to inhibit angiotensin converting enzyme. Therefore, soybean germination and fermentation could affect the concentration of bioactive compounds with angiotensin converting enzyme inhibitory properties. Conflict of interest:The authors declare no conflict of interest. &nbsp

Cannabinoids and their therapeutic applications in mental disorders

Open Access via PubMed Acknowledgments/Disclosures: This work was supported in part by funds from the Department of Biomedical Sciences Project (RICDIP_2012_Fratta_01), University of Cagliari. The authors declare no conflict of interest.Peer reviewedPublisher PD

Influenza della temperatura di essiccamento sui polifenoli e sulla capacità antiossidante delle susine Stanley

Changes in phenolic content, antioxidant capacity and ascorbic acid in prunes dried at 85°C and 60°C, were studied. Results obtained showed a significant decrease for ascorbic acid. It has to be highlighted that drying at 85°C resulted in keeping the polyphenolic pool and sharply raising the antioxidant activity, while the opposite happened for plums dried at 60°C. Lo studio ha riguardato l'evoluzione dei composti fenolici e dell'attività antiossidante di susine della varietà Stanley in seguito all’essiccamento a due temperature. Sui frutti freschi ed essiccati sono stati analizzati i composti fenolici, l’acido ascorbico e la capacità antiossidante. I risultati ottenuti hanno evidenziato un decremento significativo dell’acido ascorbico nei campioni essiccati. Si evidenzia che l’uso di un’alta temperatura porta ad un mantenimento della componente polifenolica ed a un aumento di oltre 9 volte dell’attività antiossidante in vitro, rispetto ai frutti freschi, mentre nelle susine essiccate a 60°C si ha una diminuzione di entrambi i parametri

Induction of Activity-Regulated Cytoskeleton-Associated Protein and c-Fos Expression in an Animal Model of Anorexia Nervosa

Anorexia nervosa (AN) is a complex eating disorder characterized by reduced caloric intake to achieve body-weight loss. Furthermore, over-exercise is commonly reported. In recent years, animal models of AN have provided evidence for neuroplasticity changes in specific brain areas of the mesocorticolimbic circuit, which controls a multitude of functions including reward, emotion, motivation, and cognition. The activity-regulated cytoskeleton-associated protein (Arc) is an immediate early gene that modulates several forms of synaptic plasticity and has been linked to neuropsychiatric illness. Since the role of Arc in AN has never been investigated, in this study we evaluated whether the anorexic-like phenotype reproduced by the activity-based anorexia (ABA) model may impact its expression in selected brain regions that belong to the mesocorticolimbic circuit (i.e., prefrontal cortex, nucleus accumbens, and hippocampus). The marker of neuronal activation c-Fos was also assessed. We found that the expression of both markers increased in all the analyzed brain areas of ABA rats in comparison to the control groups. Moreover, a negative correlation between the density of Arc-positive cells and body-weight loss was found. Together, our findings suggest the importance of Arc and neuroplasticity changes within the brain circuits involved in dysfunctional behaviors associated with AN

Systemic Administration of Orexin a Loaded Liposomes Potentiates Nucleus Accumbens Shell Dopamine Release by Sucrose Feeding

Orexin neurons originate in the lateral and dorsomedial hypothalamus and perifornical area and produce two different neuropeptides: orexin A (OxA) and orexin B (OxB), which activate OxR1 and OxR2 receptors. In the lateral hypothalamus (LH) orexin neurons are involved in behavior motivated by natural rewards such as palatable food (sugar, high-fat food) and it has been demonstrated similarly that the orexin signaling in the ventral tegmental area (VTA) is implicated in the intake of high-fat food. The VTA is an important area involved in reward processing. Given the involvement of nucleus accumbens (NAc) shell dopamine (DA) in motivation for food, we intended to investigate the effect of OxA on the basal and feeding-activated DA transmission in the NAc shell. OxA is a large peptide and does not cross the blood–brain barrier and for this reason was loaded on two kinds of liposomes: anti-transferrin-monoclonal antibodies (OX26-mAb) and lactoferrin-modified stealth liposomes. The effect of IV administration of both OxA liposomes on NAc shell DA was studied by microdialysis in freely moving rats. OxA, administered using both kinds of liposomes, produced a delayed and transitory increase in dialysate DA in the NAc shell, strongly and lastingly potentiated the increase in dialysate DA elicited by sucrose pellet consumption and increased the number of eaten pellets. These effects of OxA on DA transmission and feeding were prevented by the OxR1 antagonist SB 334867. Hence, OxA acting on VTA OxR1 can facilitate sucrose-stimulated NAc shell DA transmission directly by increasing the basal activity of VTA DA neurons that send their projections to the NAc shell

Effetto dell’estrazione a basso impatto ossidativo sulla capacità antiossidante <i>in vitro</i> e sulla qualità di oli extra-vergini di oliva della Sardegna

Milling technology has a great effect on the quality of olive oils. This paper was aimed to compare the differences in quality between two Sardinian extra virgin monovarietal oils obtained with a traditional and with a low oxidative stress technology. Peroxide value and acidity were lower in oils extracted with a low oxidative stress, which resulted in up to 114% higher total phenol content, with respect to oils obtained with the traditional technology. The low oxidative stress technology, moreover, permitted them to have significantly higher values of antioxidant activity, which is to be ascribed to the higher phenol content

Co-Loading of Ascorbic Acid and Tocopherol in Eudragit-Nutriosomes to Counteract Intestinal Oxidative Stress

The present study aimed at developing a new vesicular formulation capable of promoting the protective effect of ascorbic acid and tocopherol against intestinal oxidative stress damage, and their efficacy in intestinal wound healing upon oral administration. A pH-dependent copolymer (Eudragit® L100), a water-soluble prebiotic fibre (Nutriose® FM06), a phospholipid mixture (Lipoid S75), and two natural antioxidants (ascorbic acid and tocopherol) were combined to fabricate eudragit-nutriosomes by a simple, solvent-free procedure. The vesicles were spherical and oligolamellar, with some multicompartment structures in Eudragit-nutriosomes, small in size (~100 nm), with highly negative zeta potential. The effect of Eudragit® and Nutriose® on the stability on storage and in simulated gastrointestinal fluids were confirmed by the Turbiscan® technology and in vitro studies, respectively. Eudragit-nutriosomes exhibited a protective effect against H2O2-induced oxidative stress, and a proliferative effect in Caco-2 cells, as they provided the closure of the scratched area after 96 h of incubation. Keywords: Eudragit, Nutriose, phospholipid vesicles, antioxidant, intestinal wound healin

Innovative strategies to treat skin wounds with mangiferin: fabrication of transferosomes modified with glycols and mucin

im: The moisturizing properties of glycerol, the penetration enhancing capability of propylene glycol and the bioadhesive properties of mucin were combined to improve the carrier capabilities of transfersomes and the efficacy of mangiferin in the treatment of skin lesions. Materials & methods: Mangiferin was incorporated in transfersomes and glycoltransfersomes, which were also modified with mucin. The physico-chemical features were assessed, along with the efficacy against oxidative stress and skin wounds in vitro and in vivo. Results: Glycoltransfersomes promoted the deposition of mangiferin in epidermis and dermis, protected fibroblasts from oxidative stress and stimulated their proliferation. The wound healing and anti-inflammatory efficacy of glycoltransfersomes were confirmed in vivo. Conclusion: Results confirmed the potential of glycoltransfersomes in preventing/treating of skin lesions