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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >Peptide-based cationic molecules for the production of positive charged liposomes and micelles
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Peptide-based cationic molecules for the production of positive charged liposomes and micelles

机译:用于生产带正电荷的脂质体和胶束的基于肽的阳离子分子

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This paper describes the synthesis and the physico-chemical characterization of cationic peptides (CPs) for possible application as non-viral gene delivery systems. Particularly, the production of cationic liposomes and micelle solutions was considered. Liposomes were prepared by REV-phase and extrusion presenting an average diameter reflecting the pore size of the membrane used for the extrusion. After DNA complexation the mean diameter of complexes decreased by increasing the number of positive charges. The non-complexed liposome preparations showed a net positive zeta potential comprised between 17.8-30 mV. After adding Defibrotide (DFT) to liposomes (at a 1:4 ± molar ratio) the zeta potential fell down to a net negative value indicating the formation of the ionic complex. Concerning micelles, before complexation it was not possible to measure their size by PCS. However, after DFT complexation the size of complexes highly increased. In addition, as previously seen for liposomes, before complexation, the five CPs solutions showed a positive zeta potential ranging from 10-17.8 mV, while after addition of DFT the zeta potential fell to negative values. Concerning toxicity studies, in general CP-liposomes displayed a lower toxicity towards K562 cells as compared to the corresponding CP-solution. Taking into account these results, the studied CPs could be efficiently used to obtain both cationic liposomes and micelles. Moreover they are able to complex DNA with different interaction strength, depending on the type of peptide-based cationic molecule used.
机译:本文描述了阳离子肽(CPs)的合成和理化特性,可能作为非病毒基因传递系统应用。特别地,考虑了阳离子脂质体和胶束溶液的生产。通过REV相和挤出制备脂质体,其呈现出反映用于挤出的膜的孔径的平均直径。 DNA络合后,络合物的平均直径通过增加正电荷数而减小。非复合脂质体制剂显示出介于17.8-30 mV之间的净正ζ电势。在将去纤罗肽(DFT)加入脂质体(摩尔比为1:4)后,ζ电位下降至净负值,表明形成了离子络合物。关于胶束,在络合之前无法通过PCS测量其大小。但是,DFT络合后,络合物的大小大大增加。另外,如先前对于脂质体所见,在复合之前,五种CPs溶液显示的正Zeta电位范围为10-17.8 mV,而添加DFT后的Zeta电位降至负值。关于毒性研究,与相应的CP溶液相比,一般而言CP脂质体对K562细胞的毒性较低。考虑到这些结果,所研究的CP可以有效地用于获得阳离子脂质体和胶束。而且,它们能够以不同的相互作用强度复合DNA,具体取决于所使用的基于肽的阳离子分子的类型。

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