Advanced Subcompartmentalized Microreactors: Polymer Hydrogel Carriers Encapsulating Polymer Capsules and Liposomes

The design of compartmentalized carriers for advanced drug delivery systems or artificial cells and organelles is of interest for biomedical applications. Herein, a polymer carrier microreactor that contains two different classes of subcompartments, multilayered polymer capsules and liposomes, is presented. 50 nm‐diameter liposomes and 300 nm‐diameter polymer capsules are encapsulated into a larger polymer carrier capsule, demonstrating control over the spatial positioning of the subcompartments, which are either ‘membrane‐associated’ or 'free‐floating’ in the aqueous interior. Selective and spatially dependent degradation of the 300 nm‐diameter subcompartments (without destroying the structural integrity of the enzyme‐loaded liposomes) is also shown, by performing an encapsulated enzymatic reaction using the liposomal subcompartments. These findings cover several important aspects toward the development of engineered compartmentalized carrier vessels for the creation of artificial cell mimics or advanced therapeutic delivery systems.     

Targeted Liposome‐Loaded Microbubbles for Cell‐Specific Ultrasound‐Triggered Drug Delivery

One of the main problems in cancer treatment is disease relapse through metastatic colonization, which is caused by circulating tumor cells (CTCs). This work reports on liposome‐loaded microbubbles targeted to N‐cadherin, a cell–cell adhesion molecule expressed by CTCs. It is shown that such microbubbles can indeed bind to N‐cadherin at the surface of HMB2 cells. Interestingly, in a mixture of cells with and without N‐cadherin expression, binding of the liposome‐loaded microbubbles mainly occurs to the N‐cadherin‐expressing cells. Importantly, applying ultrasound results in the intracellular delivery of a model drug (loaded in the liposomes) in the N‐cadherin‐expressing cells only. As described in this paper, such liposome‐loaded microbubbles may find application as theranostics and in devices aimed for the specific killing of CTCs in blood.     

The identification and characterization of fusogenic domains in herpes virus glycoprotein B molecules

The molecular mechanism of entry of herpes viruses requires a multicomponent fusion system. Virus entry and cell-cell fusion of Herpes simplex virus (HSV) requires four glycoproteins: gD, gB and gH/gL. The role of gB remained elusive until recently, when the crystal structure of HSV-1 gB became available. Glycoprotein B homologues represent the most highly conserved group of herpes virus glycoproteins; however, despite the high degree of sequence and structural conservation, differences in post-translational processing are observed for different members of this virus family. Whereas gB of HSV is not proteolytically processed after oligomerization, most other gB homologues are cleaved by a cellular protease into subunits that remain linked through disulfide bonds. Proteolytic cleavage is common for activation of many other viral fusion proteins, so it remains difficult to envisage a common role for different herpes virus gB structures in the fusion mechanism. We selected bovine herpes virus type 1 (BoHV-1) and herpes simplex virus type 1 (HSV-1) as representative viruses expressing cleaved and uncleaved gBs, and have screened their amino acid sequences for regions of highly interfacial hydrophobicity. Synthetic peptides corresponding to such regions were tested for their ability to induce the fusion of large unilamellar vesicles and to inhibit herpes virus infection. These results underline that several regions of the gB protein are involved in the mechanism of membrane interaction.     

Characterization,Stability, and In Vitro Release Evaluation of Carboxymethyl Chitosan Coated Liposomes Containing Fish Oil

Fish oil was extracted and refined from Nile tilapia viscera. Uncoated liposomes (un‐L) and carboxymethylchitosan (CMCS)‐coated liposomes (CM‐L) containing fish oil were prepared, and their characteristics, stability, and release in vitro were studied. The CMCS coating increased the mean diameter of liposomes but there was no effect on entrapment efficiency. The surface structure and characteristics of liposomes were determined. The Fourier transform infrared spectroscopy showed that the hydrogen bonding formed between the CMCS and the carbonyl region of the liposomes’ bilayer. The transition temperature of CM‐L was higher than un‐L. The stabilities of un‐L and CM‐L stored at 4 °C were better than 25 °C. Moreover, the CM‐L was significantly more stable than un‐L when stored at 25 °C. The release behaviors of un‐L and CM‐L were governed by 2 distinct stages and the first‐order model was the most suitable model for the whole release procedure. The diffusion and erosion may be the main release mechanisms for the full controlled release of fish oil from the liposomes. This study can provide theories and practice information for further applications of fish oil from tilapia viscera.     

Improved assay of coenzyme Q10 from liposomes by Tween 80 solubilisation and UV spectrophotometry

The encapsulated coenzyme Q₁₀ (CoQ₁₀) level is an important index in evaluating the quality of CoQ₁₀ liposomes. This study demonstrates a simple method to release encapsulated CoQ₁₀ from liposomal suspension using moderate amounts of the non‐ionic surfactant Tween 80 to form mixed micelles containing phospholipids, Tween 80 and CoQ₁₀. The encapsulated CoQ₁₀ level was detected by means of Tween 80 solubilisation and ultraviolet (UV) spectrophotometry, in which 1 mL of the reducing agent NaBH₄ (7 mg mL^?1) was added. The proposed method had a good linear correlation with ethanol solubilisation and reverse phase high‐performance liquid chromatography (RP‐HPLC) and with ethanol solubilisation and UV spectrophotometry over a CoQ₁₀ concentration range of 2.5–50 µg mL^?1 (R² > 0.999). The average recovery rate of CoQ₁₀ from blank liposomes was estimated as 99.46 ± 1.54%. The difference in results between the organic solvent extraction method and the Tween 80 solubilisation method was not statistically significant (P > 0.05). When the latter method was applied to determine the total and the encapsulated CoQ₁₀ content quantitatively, the relative standard deviation was lower than 5%. Therefore this method has proved to be convenient, sensitive, accurate and reproducible compared with conventional RP‐HPLC analysis and UV spectrophotometry with organic solvent extraction. Copyright © 2006 Society of Chemical Industry     

In vitro and in vivo antioxidant properties of the plant-based supplement greens+™

Dietary antioxidants play an important role against oxidation, an underlying mechanism in the incidence of chronic diseases. Greens+ is a commercially available preparation containing a variety of plant-derived ingredients. The aim of the current study was to evaluate the antioxidant potential of the methanolic extract of greens+ powder using in vitro and in vivo techniques. In vitro studies were conducted using a liposome model system to simulate biological cell membranes. Total antioxidant potential and polyphenol content of the herbal preparation was measured. For in vivo analysis, 10 healthy human subjects consumed either three or six teaspoons of greens+ per day for four weeks. Blood samples were analyzed at baseline and at the conclusion of the treatment period for total antioxidant capacity, polyphenol content, protein, lipid and LDL oxidation, and the level of glutathione peroxidase. Results showed that greens+ supplementation was well tolerated and increased serum antioxidant potential at higher levels of intake in a dose-dependent manner. HPLC analysis showed the presence of quercetin, apigenin, kaempferol and luteolin in the supplement. Plasma analysis indicated the presence of kaempferol only. A statistically significant (p < 0.05) reduction in protein and lipid oxidation was observed. Based on its antioxidant properties, the results suggest that greens+ might play a role in reducing the risk of chronic diseases involving a burden of oxidative damage.     

血红素铁脂质体的制备

目的：制备血红素铁脂质体。方法：采用乙醇注入法及旋转薄膜- 超声法制备,再经过不同孔径的滤膜得到不同粒径的血红素铁脂质体,在原有技术的基础上优化血红素铁脂质体各组分的制备工艺,应用紫外分光光度计测定血红素铁的含量,计算出血红素铁脂质体的包封率,用差示扫描量热法检测血红素铁脂质体各组成物质的相变过程。结果：两种方法都能够得到较为理想的脂质体,血红素铁:胆固醇:卵磷脂质量比范围为(0.1～200):(1～10):(10～100)。结论：所得血红素铁脂质体呈均一大单室型,通过0.8μm 的滤膜后有效粒径为0.804μm,最大包封率36%。     

蛋黄卵磷脂的结构、提取、功能与脂质体研究进展

综述蛋黄卵磷脂的分子结构、提取方法、功能活性,以及在脂质体方面的最新研究现状。蛋黄卵磷脂结构主要是以甘油为骨架,通过酰基键与磷酸和脂肪酸连接而成的一种磷脂类两亲分子,根据碱基基团的不同,蛋黄卵磷脂包括了磷脂酰胆碱、磷脂酰乙醇胺、磷脂酰肌醇、磷脂酰丝氨酸、磷脂酸和磷脂酰甘油等6种。目前,提取蛋黄卵磷脂的方法主要有溶剂提取法和超临界萃取法;蛋黄卵磷脂具有抗氧化、抗菌、抗炎、神经保护和心脑血管保护等功能的生理活性;此外,还简单介绍了蛋黄卵磷脂脂质体的种类和应用现状。为蛋黄卵磷脂产品的开发提供良好的参考。