Chemical,amino acid and fatty acid composition of Sterculia urens L. seed

The chemical, amino acid and fatty acid compositions of Sterculia urens seeds are reported. The cotyledons were found to be rich in protein (30.88%) and lipids (39.2%). The major amino acids in defatted Sterculia urens cotyledon flour (DSCF) were determined as glutamic acid, arginine and aspartic acid. Cysteine, methionine, tyrosine and histidine were observed in minor quantities. The ratio of essential to non-essential amino acids was observed to be 0.45. Among the essential amino acids, isoleucine was found to be higher than the reported FAO/WHO requirements. The GC-FID and GC–MS analysis revealed that the major fatty acids of the total lipid were stearic acid (31.72%), linoleic acid (28.83%) and palmitic acid (26.79%). Eicosadienoic acid (4.98%) and eicosatrienoic acid (2.96%) were also found in the total lipid.     

Amphiphilic drug interactions with model cellular membranes are influenced by lipid chain-melting temperature

Small-molecule amphiphilic species such as many drug molecules frequently exhibit low-to-negligible aqueous solubility, and generally have no identified transport proteins assisting their distribution, yet are able to rapidly penetrate significant distances into patient tissue and even cross the blood–brain barrier. Previous work has identified a mechanism of translocation driven by acid-catalysed lipid hydrolysis of biological membranes, a process which is catalysed by the presence of cationic amphiphilic drug molecules. In this study, the interactions of raclopride, a model amphiphilic drug, were investigated with mixtures of biologically relevant lipids across a range of compositions, revealing the influence of the chain-melting temperature of the lipids upon the rate of acyl hydrolysis.     

Solid lipid nanoparticles of anticancer drug andrographolide: formulation,in vitro and in vivo studies

Diterpenoidal anti-cancer drug andrographolide (AD) was encapsulated into solid lipid nanoparticle (SLN) because of poor aqueous solubility and high lipophilicity. AD-SLNs were prepared by solvent injection method and characterized for droplet size, surface morphology, zeta potential, etc. In vitro drug release was carried out by dialysis-membrane method. A pharmacokinetic study was performed by UPLC/Q-TOF-MS method to determine the maximum plasma concentration (C_max), area under the curve (AUC), etc. There was an improvement in C_max and AUC of AD-SLNs when compared with AD, thereby enhancing the bioavailability of AD. The t_max was increased than that of AD suspension, indicating the sustained release pattern of AD-SLNs. The antitumor activity was carried out on Balb/c mice showing better results with AD-SLNs as compared to AD. Thus, the AD-loaded SLNs would be useful for delivering poorly water-soluble AD with enhanced bioavailability and improved antitumor activity.     

Preparation and evaluation of Baicalin-loaded cationic solid lipid nanoparticles conjugated with OX26 for improved delivery across the BBB

Purpose: A novel brain targeting drug delivery system based on OX26 antibody conjugation on PEGylated cationic solid lipid nanoparticles (OX26-PEG-CSLN) was prepared.

Methods: The Baicalin-loaded PEGylated cationic solid lipid nanoparticles modified by OX26 antibody (OX26-PEG-CSLN) were prepared by emulsion evaporation–solidification at low temperature method. The immune-gold labeled OX26-PEG-CSLN was visualized by transmission electron microscopy. The mean diameter and zeta potential of OX26-PEG-CSLN, PEG-CSLN and CSLN were determined using a Zetasizer. The entrapment efficiency of OX26-PEG-CSLN, PEG-CSLN and CSLN was determined by ultrafiltration centrifugation method. And the solid-state characterization of OX26-PEG-CSLN and CSLN were analyzed by X-ray. Pharmacokinetics studies were conducted by in vivo microdialysis in rat cerebrospinal fluid.

Results: The results showed that the OX26-PEG-CSLN, PEG-CSLN and CSLN had average diameters of 47.68?±?1.65, 27.20?±?1.70 and 33.89?±?5.74?nm, Zeta potentials of ?0.533?±?0.115?mV, 11.200?±?0.500?mV and 11.080?±?1.170?mV and entrapment efficiencies of 83.03?±?0.01%, 92.90?±?3.50% and 97.83?±?0.19%, respectively. In the pharmacokinetics studies, the AUC value of OX26-PEG-CSLN was11.08-fold higher than that of the Baicalin solution (SOL) (p?p?>?0.05); the C_max value of OX26-PEG-CSLN was 7.88-fold higher than that of SOL (p?p?Conclusion: These results demonstrated OX26-PEG-CSLN could be a promising carrier to deliver drugs across the BBB for the treatment of brain diseases.     

壳聚糖季铵盐修饰的辅酶Q10纳米结构脂质载体的制备及表征

为了增强运载辅酶Q10的纳米结构脂质载体(CoQ10-NLC)的透皮效果,采用促渗剂——壳聚糖季铵盐(QCS)对CoQ10-NLC进行了表面修饰,并结合QCS分子链的自聚集行为,明确了壳聚糖季铵盐修饰的包载辅酶Q10的纳米脂质体(QCS-CoQ10-NLC)的形成机制,得到了粒径在500 nm左右的脂质载体。进一步通过体外透皮实验,考察了QCS-CoQ10-NLC的透皮吸收效果。结果显示,经质量分数0.5%的QCS修饰后,脂质载体可将CoQ10在皮肤中的渗透总量由1.36μg/cm~2显著增加至5.14μg/cm~2。     

Effects of three conventional drying methods on the lipid oxidation,fatty acids composition,and antioxidant activities of walnut (Juglans regia L.)

Three walnut (Juglans regia L.) drying methods (sun drying, direct oven drying, and intermittent oven drying) were employed, and the consequent changes in lipid oxidation attributes, such as acid value (AV), peroxide value (POV), saponification value (SV), fatty acid composition, and antioxidant activity [including reducing power, superoxide anion scavenging activity, 1,1-diphenyl-2-picrylhydrazyl free radical scavenging activity (DPPH), lipoxygenase (LOX) activity, total phenols content (TPC), and total flavonoids content (TFC)] were investigated in this study. Sun drying resulted in the highest AV, POV, and SV, followed by direct oven drying and intermittent oven drying. Antioxidant activities and related compounds, TPC and TFC, were initially increased and then declined during drying, and a significant correlation was found between antioxidant activity and TPC and TFC. The LOX activities of all samples showed an increasing trend, although those of the sun-dried samples were the lowest. The walnuts dried with the intermittent oven drying method contained more linoleic acid than those dried by direct oven drying. Overall, intermittent oven drying appears to be a promising strategy for fresh walnut drying.     

Low n-6/n-3 PUFA Ratio Improves Lipid Metabolism,Inflammation, Oxidative Stress and Endothelial Function in Rats Using Plant Oils as n-3 Fatty Acid Source

Lipid metabolism, inflammation, oxidative stress and endothelial function play important roles in the pathogenesis of cardiovascular disease (CVD), which may be affected by an imbalance in the n‐6/n‐3 polyunsaturated fatty acid (PUFA) ratio. This study aimed to investigate the effects of the n‐6/n‐3 PUFA ratio on these cardiovascular risk factors in rats fed a high‐fat diet using plant oils as the main n‐3 PUFA source. The 1:1 and 5:1 ratio groups had significantly decreased serum levels of total cholesterol, low‐density lipoprotein cholesterol, and proinflammatory cytokines compared with the 20:1 group (p < 0.05). Additionally, the 20:1 group had significantly increased serum levels of E‐Selectin, von Willebrand factor (vWF), and numerous markers of oxidative stress compared with the other groups (p < 0.05). The 1:1 group had a significantly decreased lipid peroxide level compared with the other groups (p < 0.05). Serum levels of malondialdehyde, reactive oxygen species and vWF tended to increase with n‐6/n‐3 PUFA ratios increasing from 5:1 to 20:1. We demonstrated that low n‐6/n‐3 PUFA ratio (1:1 and 5:1) had a beneficial effect on cardiovascular risk factors by enhancing favorable lipid profiles, having anti‐inflammatory and anti‐oxidative stress effects, and improving endothelial function. A high n‐6/n‐3 PUFA ratio (20:1) had adverse effects. Our results indicated that low n‐6/n‐3 PUFA ratios exerted beneficial cardiovascular effects, suggesting that plant oils could be used as a source of n‐3 fatty acids to prevent CVD. They also suggested that we should be aware of possible adverse effects from excessive n‐3 PUFA.