In the present study, a novel nonionic surfactant vesicles (NSVs) system consisting of cholesterol, Tween 80 and Span 80 was developed for the delivery of Ginsenoside Rb-1 with an improved oral bioavailability. The prepared vesicles were hollow and spherically shaped with acceptable diameter (264.68 +/- 4.17 nm), zeta potential (-11.58 +/- 0.87 mV) and encapsulation efficiency (69.034 +/- 0.045%). XRD analysis provided affirmed the encapsulation of Rb-1 in the vesicles. The in vitro release profile of Rb-1 from the vesicles in the two different media (double distilled water, pH 7.0, phosphate buffer solution, pH 7.4) showed statistical insignificant difference when compared with the free Ginsenoside Rb-1. Notably, the pharmacokinetic analysis of optimized Ginsenoside Rb-1-NSVs exhibited a higher C-max (9.55 +/- 0.5 mu g/mL versus 6.22 +/- 0.53 mu g/mL) with 1.82-fold increase in relative oral bioavailability. Collectively, these findings revealed that the developed vesicles could be a novel alternative in improving the oral bioavailability of Ginsenoside Rb-1 and extending its application in the clinical setting.

Abstract This study aimed to investigate structural features and antihyperlipidemic effects of the stigma maydis polysaccharide, termed SMP‐1. This polysaccharide was composed of D‐mannose, L‐rhamnose, D‐glucose, D‐galactose, L‐arabinose, D‐xylose, and D‐galacturonic acid, with a molar ratio of 1.00:0.21:1.41:1.44:0.70:0.44:0.56. The SMP‐1 was mainly bonded by (1 → 6) and (1 → 3) linkages, with various monosaccharides being evenly distributed in the main and side chains. Moreover, SMP‐1 had neither triple‐helical structure nor molecular aggregation. Importantly, the SMP‐1 could effectively bind the bile acids in vitro and significantly lower the total cholesterol, triglyceride, low‐density lipoprotein cholesterol levels, and moderately increase the high‐density lipoprotein cholesterol level in poloxamer 407‐induced hyperlipidemic mice. Moreover, pretreatment with SMP‐1 (≥300 mg/kg) could remarkably reduce fat accumulation and restore hepatocyte morphology in the liver of hyperlipidemic mice. Altogether, these findings indicated that SMP‐1 could be developed as a safe and effective food supplement for preventing and treating hyperlipidemic disorders.

The study was aimed at formulating self-assembled capsaicin prodrug nanoparticles (Cap-SSVE NPs) with improved bioavailability, increased antihyperlipidemic activity and less gastrointestinal mucosa irritations. The in vitro release profile of the developed Cap-SSVE NPs was stable in HCl solution (pH 1.2) and distilled water, but very susceptible in PBS (pH 6.8 and 7.4). The relative oral bioavailability of Cap-SSVE NPs was 3.2 folds higher than free capsaicin, with an extended Tmax (0.25–1 h). The Cap-SSVE NPs decreased certain lipid profile indices of both the liver tissue (Total lipids and TG) and the blood sample (TC, TG, LDL and TBA) with elevated levels of HDL in high fat diet induced hyperlipidemic rats. The nanoparticles also predominantly accumulated in the liver with reduced irritations in the gastrointestinal mucosa. Collectively, the formulated Cap-SSVE NPs showed an enhanced bioavailability, increased hypolipidemic effects and reduced mucosa irritations.

目的:研究玉米须酸性多糖(acid corn silk polysaccharide,ACSP)的基本结构特征,并探究其对体内血脂的影响.方法:玉米须经水提醇沉提取,所得粗多糖经D315大孔阴离子交换树脂和葡聚糖凝胶柱Sephadex G100分离纯化,得到组分ACSP,并对其进行结构表征.将42只小鼠分为对照组、模型组、ACSP高剂量(500 mg·kg-1)和低剂量(100 mg·kg-1)组以及2个阳性对照组,每组7只,采用高脂饲料构建高血脂小鼠模型;各组对应处理30 d后,测定血浆总胆固醇、三酰甘油、低密度脂蛋白胆固醇(LDL-C)和高密度脂蛋白胆固醇(HDL-C).结果:20 g玉米须粗多糖经分离纯化得到ACSP 4.3354 g,收率约为21.68%.ACSP是由D-甘露糖、L-鼠李糖、D-葡萄糖醛酸、D-葡萄糖、D-半乳糖、L-阿拉伯糖、D-木糖等7种单糖组成的杂聚糖;糖含量和单糖组成测定结果均显示ACSP是酸性糖,糖醛酸含量为(37.00±1.03)%;分子量约为19.32 kD;红外光谱显示典型的多糖吸收峰并具有糖醛酸的羧基特征吸收峰;刚果红试验显示ACSP为非三螺旋结构.与模型组相比,500 mg·kg-1 ACSP组血脂水平明显改善(P<0.05).结论:本实验分离纯化得到的ACSP是由7种单糖组成的非三螺旋结构酸性糖,具有显著的降血脂活性.

Hypolipidemic polysaccharides have notable activity and safety with a range of diverse sources. In this paper, the classification of hypolipidemic polysaccharides was carried out into polysaccharide sulfate, glycosaminoglycan, homopolysaccharide and heteropolysaccharide. The hypolipidemic activity mechanism and structure-activity relationship hypothesis of those polysaccharides in recent years were briefly reviewed therefore to provide references for the study and product development of polysaccharides.

Summary This study is focused on the isolation and characterisation of two purified polysaccharide fractions (namely PPEP ‐1 and PPEP ‐2) from Pleurotus eryngii ( P. eryngii ) and evaluation of their hypolipidaemic effects. The Congo red analysis indicated that PPEP ‐2 but not PPEP ‐1 possessed a triple‐helix conformation. The atomic force microscope analysis revealed that PPEP ‐1 and PPEP ‐2 showed different polysaccharide chain conformations. Importantly, the mice treated with PPEP ‐1 showed significantly lowered serum levels of total cholesterol ( TC ), triglyceride ( TG ) and low‐density lipoprotein cholesterol ( LDL ‐c) and increased high‐density lipoprotein cholesterol when compared with the hyperlipidaemia mice induced by the high‐fat diet. However, PPEP ‐2 revealed less hypolipidaemic effect than PPEP ‐1. Additionally, both PPEP ‐1 and PPEP ‐2 demonstrated remarkable hypolipidaemic effects by decreasing levels of serum TC , TG and LDL ‐c in the hyperlipidaemic model induced by P‐407. Taken together, our findings suggest that the P. eryngii polysaccharides, especially PPEP ‐1, could be developed as a natural functional food supplement for preventing hyperlipidaemia.

Ginkgo biloba extract (GBE50), the fifth generation extract of Ginkgo biloba, has been widely used in clinical treatment. This study was aimed at developing self-microemulsifying drug delivery system sustained-release pellets (SMEDDS-SR pellets) to achieve sustained release and increased the oral bioavailability of GBE50. Solubility studies and Pseudo-ternary phase diagrams were investigated to optimize the suitable compositions of SMEDDS-SR pellets. The optimal formulation of GBE50-SMEDDS consisting of oil (16.7% MCT), surfactant (33.4% Cremophor EL35), cosurfactant (33.4% PEG 400) and drug (16.7% GBE50) was obtained. The GBE50-SMEDDS-SR pellets were prepared by mixing GBE50-SMEDDS with diluent agent (MCC), disintegration agent (PVPP) and coating material of ethyl cellulose (EC) using extrusion spheronization method. The Morphology study of GBE50-SMEDDS-SR pellets after dispersion in water revealed a spherical and homogeneous structure of droplets (51.6 +/- 1.8) nm. The in vitro release data revealed the sustained-release effect of GBE50-SMEDDS-SR pellets. Pharmacokinetics study in beagle dogs after oral administration yielded relative bioavailability (Fr) of 160.24% and 236.18% for GBE50-SMEDDS and GBE50-SMEDDS-SR pellets, respectively. Collectively, these results indicated that the SMEDDS-SR pellets could be an effective delivery system to achieve sustained release and improved oral bioavailability of GBE50. (C) 2017 Elsevier B.V. All rights reserved.