磷脂酰胆碱三酯的结构及其对模型哺乳动物膜理化性质影响的相关性研究。

IF 4.6 Q2 MATERIALS SCIENCE, BIOMATERIALS ACS Applied Bio Materials Pub Date : 2023-11-20 DOI:10.1016/j.bbamem.2023.184254
Marzena Mach , Łukasz Płachta , Paweł Wydro
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引用次数: 0

摘要

阳离子脂质是一种具有两亲性的合成化合物,作为遗传物质的载体,广泛应用于药物传递系统,特别是基因治疗中。众所周知,阳离子脂类在DDS中应用的主要限制是它们体内给药后的高细胞毒性和低生物活性。这可能与脂质结构与活性之间的关系以及脂质感染或给药机制尚不完全清楚有关。因此,在这项工作中,我们确定了一组阳离子脂质-磷脂酰胆碱三酯(Et-PCs) -不同的疏水结构对模型哺乳动物膜的影响。本研究采用朗缪尔单层膜和脂质体作为模型体系。结果表明,Et-PCs掺入模型哺乳动物膜后,脂质间的相互作用减弱,导致膜的流动性、无序度和通透性增加。以这种方式破坏膜的稳定性可以促进药物进入,携带在阳离子脂质体内,进入病理细胞。此外,研究证明阳离子脂质疏水部分的结构也会影响脂质膜的性能。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Study of the correlation between the structure of selected triester of phosphatidylcholine and their impact on physicochemical properties of model mammalian membranes

Cationic lipids are synthetic compounds of amphiphilic character used in Drug Delivery Systems (DDS), especially in gene therapy, as the carriers of genetic material. As it is known, the main limitation of the application of cationic lipids in DDS is their high cytotoxicity after in vivo administration and low bioactivity. This is probably related to not fully known the relationship between the lipid structure and its activity as well as the mechanism of lipofection or drug delivery. Therefore, in this work we determined the impact of a selected group of cationic lipids - triesters of phosphatidylcholine (Et-PCs) - differing in their hydrophobic structure on model mammalian membranes. In the research, as model systems, Langmuir monolayers and liposomes were applied. It was shown that the incorporation of Et-PCs into model mammalian membranes weakens interactions between lipids, causing the increase of fluidity, disordering degree and permeability of membrane. The destabilization of the membrane in this way can facilitate the entry of drugs, carried inside cationic liposomes, into the pathological cell. Moreover, the studies prove that the structure of the hydrophobic part of cationic lipids also affects the properties of lipid membranes.

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来源期刊
ACS Applied Bio Materials
ACS Applied Bio Materials Chemistry-Chemistry (all)
CiteScore
9.40
自引率
2.10%
发文量
464
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