Retention of topical liposomal formulations on the cornea

Summary The ability of liposomes composed of different kinds of phospholipid materials to adhere to the surface of the cornea was studied in the rabbit. The liposomes were labelled with tracer amounts of an I¹²⁵-labelled phosphatidylethanolamine derivative and were instilled in 10 l drops onto the cornea. The retention of radioactivity was monitored. The results show that liposomes containing positively charged phospholipids are better retained than an albumin control. Thus, it may be possible to develop a drug delivery, liposome system which would permit long-term sustained release of ophthalmic drugs onto the cornea.     

硫酸氢黄连素脂质体的制备工艺研究

以薄膜分散-超声法制备硫酸氢黄连素(Bb)脂质体.探讨了影响Bb脂质体包封率的因素,确定了最佳处方及实验条件,使包封率达57.5%,经电镜观察所制得的脂质体为微球状的大单室脂质体.     

姜黄素长循环脂质体的制备及表征

为了改善姜黄素长循环脂质体(Cur-LCL)的稳定性,延长药物在体内的循环时间,对现有姜黄素脂质体(Cur-Lips)和姜黄素长循环脂质体的制备方法进行了优化。使用乙醇注入法制备Cur-Lips,用后插法将DSPE-PEG2000插入Cur-Lips中制成Cur-LCL。结果表明:Cur-LCL外观为圆形囊泡状球体,平均包封率为(88.91±0.94)%,4℃存放15d包封率没有明显变化,平均渗漏率为2.4%,具有较好的稳定性;Cur-LCL平均粒径为(118.4±3.2)nm(n=3),呈单峰分布,平均电位为(-12.9±0.32)mV(n=3);以溶解度为标准对溶出介质进行筛选,选择以1%Tween 80的生理盐水为体外释放试验的溶出介质,Cur原料药12h基本释放完全,Cur-Lips在36h基本释放完全,累计释放率为92.67%,Cur-LCL在72h基本释放完全,累计释放率为91.36%。Cur-LCL具有明显的缓释性,可以延长药物在血液中的循环时间,达到长循环的效果。     

大黄酚脂质体包封率测定方法的研究

目的建立大黄酚脂质体包封率的测定方法。方法采用低速离心法分离载药脂质体与游离的药物,采用紫外分光光度法测定大黄酚的含量,计算出包封率。结果实验结果表明,当离心条件为1 500r/min、离心时间为120s时,可将载药脂质体与游离药物有效地分离,并测得3批大黄酚脂质体的包封率分别为82.29%,83.25%和83.06%,符合2010版《中华人民共和国药典》的规定。结论该方法简便快速,准确可靠,可用于测定大黄酚脂质体的包封率。     

Fluorescence response of acridine orange to changes in pH gradients across liposome membranes

Summary The influence that changes in proton distribution have on the fluorescence of acridine orange was examined using negatively charged liposomes. Our results indicate that at least two mechanisms are involved: distribution of the probe between the internal aqueous phase of the liposomes and the outside medium, and binding of the probe to the liposome membranes.     

阳离子脂质体在基因治疗中的应用

介绍了阳离子脂质体的组成和结构特点以及作为基因载体在基因治疗方面的应用．阳离子脂质体转基因的机理研究表明：阳离子脂质体／基因复合物进入细胞的方式依赖于细胞的内吞作用或通过细胞的膜融合作用．     

Progress in fabricating arrays of soft spherical vessels on mesoscale with spatial control

Microarrays of spherical vessel-like colloids such as liposomes, polymerized vesicles and polyelectrolyte capsules may find diverse applications in bioanalysis, biosensing, and combinatorial chemistry, for their capabilities in encapsulating chemical species such as drugs, biomolecules, probes, polymers and nanoparticles. This review reports the advances on methods for fabricating microarrays of the various hollow colloids. Related strategies are described in detail, including patterning techniques, surface modification methods, and tethering approaches such as oligonucleotide hybridization, receptor-ligand binding, covalent coupling and electrostatic interaction. The preliminary developments of functionalities of these arrays serving as sensor chips, microcarriers and microreactors are summarized as well.     

Sulfatide-tenascin interaction mediates binding to the extracellular matrix and endocytic uptake of liposomes in glioma cells

Tenascin-C is an extracellular matrix glycoprotein, whose expression is highly restricted in normal adult tissues, but markedly up-regulated in a range of tumors, and therefore serves as a potential receptor for targeted anticancer drug or gene delivery. We describe here a liposomal carrier system in which the targeting ligand is sulfatide. Experiments with tenascin-C-expressing glioma cells demonstrated that binding of liposomes to the extracellular matrix relied essentially on the sulfatide-tenascin-C interaction. Following binding to the extracellular matrix, the sulfatide-containing liposomes were internalized via both caveolae/lipid raft- and clathrin-dependent pathways, which would ensure direct cytoplasmic release of the cargoes carried in the liposomes. Such natural lipid-guided intracellular delivery targeting at the extracellular matrix glycoproteins of tumor cells thus opens a new direction for development of more effective anticancer chemotherapeutics in future. K. Shao & Q. Hou: These authors contributed equally to this work. Received 22 September 2006; received after revision 5 December 2006; accepted 9 January 2007     

星点设计-效应面法优化羟基喜树碱-粉防己碱复方脂质体的处方

制备羟基喜树碱-粉防己碱复方脂质体,采用星点设计-效应面法,优选最佳的脂质体的制备工艺。制备羟基喜树碱-粉防己碱脂质体,通过单因素实验选出影响显著的三个因素胆脂比、水化温度、药脂比为自变量,包封率为因变量,根据Design-Expert6.0.5软件设计实验。通过线性回归、多元线性回归拟合后建立自变量与因变量之间的数学关系,根据数学模型绘制效应面及等高线图,从中选择最佳的实验方案。结果三项式拟合方程的r值较高,拟合度好,通过效应面选出的最佳制备工艺条件为胆脂比1∶6,水化温度51℃,药脂比1∶22,工艺验证结果与预测值的偏差分别为1.71%、1.89%通过星点设计-效应面法优化的制备复合脂质体的工艺条件准确可靠。     

磁感应热疗恶性肿瘤技术研究进展

 磁感应热疗恶性肿瘤是一种基于交变磁场辐照磁介质并通过磁感应产热杀死肿瘤病变组织的新兴技术。20世纪60年代,磁感应热疗技术兴起,围绕提高热疗效果、开发兼具多重疗效的磁性介质和优化温度场分布,开展了大量研究工作,取得了显著效果。本文总结了铁磁热籽、磁流体、磁性脂质体、磁性微晶玻璃、磁性骨水泥等的实验研究与临床应用近期进展,指出进一步提高疗效、优化治疗区热场分布中存在的问题。