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由脂肪酸和 N-[3-(二甲基氨基)丙基]-十八酰胺组成的囊泡:脂肪酸链长对囊泡物理化学性质的影响。

Vesicles composed of fatty acid and N-[3-(dimethylamino)propyl]-octadecanamide: effect of fatty acid chain length on physicochemical properties of vesicles.

机构信息

College of Biomedical Science and Institute of Bioscience and Biotechnology, Kangwon National University , Kangwon-do , Korea.

出版信息

Drug Dev Ind Pharm. 2014 Mar;40(3):318-24. doi: 10.3109/03639045.2012.760578. Epub 2013 Jan 30.

DOI:10.3109/03639045.2012.760578
PMID:23360361
Abstract

BACKGROUND AND OBJECTIVES

Vesicles, recently claimed as drug delivery carriers, were prepared by taking advantage of an electrostatic interaction between the carboxylic groups of fatty acids (FAs) and the amino groups of N-[3-(Dimethylamino)propyl]-Octadecanamide (DMAPODA). The study is to find out the effect of FAs' chain length on physicochemical properties of vesicles.

METHODS

Decanoic acid (DA), myristic acid (MA), stearic acid (SA) and behenic acid (BA) were used as FAs. Vesicles composed of them and DMAPODA were studied about formation on microscope, calorimetric analysis, size and zeta potential.

RESULTS

On microphotographs, all of FAs could form vesicles when mixed with DMAPODA in an equi-molar ratio. However, DA/DMAPODA vesicles were disintegrated during the homogenization. Due to the asymmetry of DA/DMAPODA associate, it seems to hardly form a stable and well-packed bilayer. On thermograms, the vesicles exhibited one strong peak, indicating that FAs can be homogeneously mixed with the cationic amphiphile. The sizes of the four kinds of vesicles suspended in an aqueous solution (final pH 7.5) were in the same order (hundreds of nanometer) on microphotographs. But, on a light scattering machine, the mean size of MA/DMAPODA vesicle was measured to be much greater than those of the other vesicles, possibly because of the low absolute value of the zeta potential. In addition, the medium pH value had a significant effect on the size of BA/DMAPODA vesicle possibly because the zeta potential was strongly dependent on the pH value.

CONCLUSION

FAs' chain length would affect the physicochemical properties of vesicles composed of them and DMAPODA.

摘要

背景与目的

囊泡最近被认为是药物传递载体,是通过利用脂肪酸(FA)的羧基与 N-[3-(二甲氨基)丙基]-十八酰胺(DMAPODA)的氨基之间的静电相互作用来制备的。本研究旨在探讨 FA 的链长对囊泡理化性质的影响。

方法

使用癸酸(DA)、肉豆蔻酸(MA)、硬脂酸(SA)和山嵛酸(BA)作为 FA。研究了它们与 DMAPODA 组成的囊泡在显微镜下的形成、量热分析、粒径和 Zeta 电位。

结果

在显微照片上,当 FA 与 DMAPODA 以等摩尔比混合时,所有 FA 都可以形成囊泡。然而,DA/DMAPODA 囊泡在均质化过程中被破坏。由于 DA/DMAPODA 配合物的不对称性,它似乎很难形成稳定且包装良好的双层。在热谱图上,囊泡显示出一个强峰,表明 FA 可以与阳离子两亲物均匀混合。在 pH 值为 7.5 的水溶液中悬浮的四种囊泡的粒径(数百纳米)在显微照片上相同。但是,在光散射仪上,MA/DMAPODA 囊泡的平均粒径明显大于其他囊泡,可能是因为 Zeta 电位的绝对值较低。此外,介质 pH 值对 BA/DMAPODA 囊泡的粒径有显著影响,可能是因为 Zeta 电位强烈依赖于 pH 值。

结论

FA 的链长会影响由它们与 DMAPODA 组成的囊泡的理化性质。

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