通过改变脂质体中磷脂成分,构建了不同电性的脂质体.利用表面活性剂介导方法,将截短的金黄色葡萄球菌细胞膜上的组氨酸激酶AgrC(AgrCTM6-7C)蛋白重构到不同电性的脂质体上.结果表明,阴离子脂质体对AgrCTM6-7C蛋白的镶嵌效率明显高于阳离子脂质体,约60%~70%镶嵌至阴离子脂质体中的AgrCTM6-7C蛋白的细胞质域朝向脂质体囊泡的外部,并保持较高活性.利用圆二色光谱比较了AgrCTM6-7C蛋白在表面活性剂胶束和脂质体中的二级结构稳定性,发现阴离子脂质体对AgrCTM6-7C蛋白的二级结构具有一定的保护作用,可明显提高蛋白的热稳定性.

AgrC is a membrane-embedded histidine kinase in Staphylococcus aureus that is thought to act as a sensor for the recognition of environmental signals and the transduction of signals into the cytoplasm so as to regulate and control a series of related pathogenic gene expression. However, for the complexity of cell mem-brane, it turns to be difficult to study AgrC on bacterial cell membrane directly. Many researches tried to take advantage of proteoliposome which could provide an approximate natural membrane environment and keep the protein activity to study the structure and function of membrane proteins. In order to build a transmembrane protein incorporation system with a relatively high incorporation efficiency, function activity and stability, various factors were considered, such as the impact of different charge polarity head on protein transmembrane incorporation efficiency. Here, four kinds of different charged liposomes were prepared by changing the phos-pholipid components in

背景 布比卡因脂质体是一种新型的酰胺类局部麻醉药,是采用脂质体技术制备而成的缓释布比卡因.研究表明,布比卡因脂质体的局部镇痛作用时间可长达72 h.目的 拟对有关布比卡因脂质体的相关研究予以综述,重点介绍其在术后镇痛方面的相关研究进展.内容 从布比卡因脂质体的特性、药动学、药效学及安全性4个方面综述布比卡因脂质体在术后镇痛中的应用.趋向 布比卡因脂质体作为超长镇痛局麻药,在术后镇痛中将具有广泛的应用价值.

Background Liposomal bupivacaine is a kind of novel amide local anesthetics,and a slow-released bupivacaine produced by liposome technology.Many studies indicated that the analgesic time of liposomal bupivacaine could persist for 72 h.Objective To review the researches related to liposomal bupivacaine,especially the progress of liposomal bupivacaine for postsurgical analgesia.Content This review described the characteristics,pharmacokinetics,pharmacodynamics and safety of liposomal bupivacaine for postsurgical analgesia.Trend As one of the local anesthetics producing ultralong-acting analgesia,the wide application of liposomal bupivacaine is quite promising in postsurgical analgesia.

目的：比较Lipofectamine2000、lipoplexes和apoE-lipoplexes三种脂质体对Li-7肝癌细胞的转染效率。方法构建普通阳离子脂质体 lipoplexes 和载脂蛋白 apoE 修饰脂质体apoE-lipoplexes；使用Lipofectamine2000，lipoplexes和apoE-lipoplexes三种脂质体运载以EGFP为报告基因的pGenesil-1质粒转染Li-7肝癌细胞，通过荧光显微镜观察EGFP蛋白的表达，流式细胞术检测三种脂质体的转染效率。结果 Lipofectamine2000、lipoplexes和apoE-lipoplexes三种脂质体转染效率分别为（18.63±0.57）%，（24.07±0.91）%，（28.93±0.50）%，3组间两两比较均有显著性差异（P＜0.01）。结论 Li-7肝癌细胞的转染效率与脂质体的结构有关，提示脂质体结构改造可能成为提高转染效率的新策略。

Objective To compare the transfection efficiency of the three kinds of liposomes, Lipofectamine2000, lipoplexes and apoE-lipoplexes on Li-7 hepatoma cells. Methods To construct two kinds of gene vectors, one was normal cationic liposome (lipoplexes), another was composed of liposomes (lipoplexes) and apolipoproteinE(apoE-lipoplexes). The plasmid pGenesil-1 containing EGFP reporter gene was transfected into Li-7 cells using Lipofectamine2000, lipoplexes and apoE-lipoplexes, respectively. Then the expression of EGFP was observed by fluorescence microscopy, and the transfection efficiency of the three kinds of liposomes was measured by flow cytometry. Results Transfection efficiency of Lipofectamine2000, lipoplexes and apoE-lipoplexes was (18.63±0.57)%, (24.07±0.91)%and (28.93±0.50)%separately with the difference being significant among them (P<0.01). Conclusion Transfection efficiency of the liposome on Li-7 hepatoma cells is related to its structures, indicating that the st

采用薄膜分散法制备大蒜多糖长循环脂质体,并对其形貌、粒径进行了表征,同时对脂质体包封率、稳定性进行了研究。结果表明:经聚乙二醇(PEG)修饰的长循环脂质体形态圆整、分散均匀,平均粒径为115.4 nm;对大蒜多糖的包封率为71.94%,明显高于普通脂质体的包封率,同时该脂质体还具有较好的稳定性。

Long circulating liposomes containing garlic polysaccharide was prepared by thin film method , and its morphology and particle size were characterized. The encapsulation efficiency and stability of liposomes were also studied. The results showed that the long circulating liposomes were relatively and regularly spherical in shape , evenly distributed and had an average particle size of 115.4 nm. The encapsulation efficiency for garlic polysaccharide reached 71.94 %, significantly higher than that of ordinary liposomes without PEG coating. Moreover, the long circulating liposomes also have good stability.

[目的]综述脂质体的应用和研究进展,为药物制成脂质体提供更多的选择。[方法]查阅近几年国内相关的文献资料并总结脂质体在各方面的应用、新的制备方法和修饰方法及其各自的优点。[结果]从脂质体的的应用、制备方法、修饰、质量评价等方面,可看脂质体与生物膜有着极好的相容性,作为载体有很大的优势,修饰后,能增强靶向性,提高药物的疗效,降低毒副作用。[结论]随着新材料的产生和新技术的发展,脂质体的优势将更加显现脂质体作为一种新型的药物载体,与生物膜具有相似性,具有多种优良特性,改变了传统的给药方式。经过近40年的研究,已到广泛的应用。

[Objective]This paper summarizes the latest literature,which can offer more choices for making liposome drug.[Methods]This article summarizes the application of liposomes in al aspects and new preparation methods and modification methods and their respective advantages. [Results]Liposome as a new type of drug carrier,which has similarity with biological membrane,has many good qualities and changes the traditional way to give medicine. [Con-clusion]Liposome has the broad application after nearly forty years of research.