脂质体形式具有硫辛酸和肌肽的产生、抗血小板和抗氧化作用

V. Shchelkonogov, O. Baranova, A. Chekanov, K. Kazarinov, N. Shastina, S. Stvolinsky, T. Fedorova, E. Solovieva, A. Fedin, G. Sorokoumova
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引用次数: 0

摘要

选择了以硫辛酸和肌肽为原料制备脂质体的最佳工艺条件。采用主动和被动负载的方法,可以实现肌肽(60±5%)和硫辛酸(75±5%)在纳米颗粒(NPs)中的高效包合。研究表明,在纳米分散体(NDs)中加入蔗糖或胆固醇(Chol)会导致肌肽在纳米颗粒中的掺入效率略有下降(45±5%)。用LA和肌肽被动负载生产pc -脂质体(PC-Ls)导致脂质体中肌肽包合效率显著降低(16%)。与此同时,采用被动和主动负载的方法,LA在PC脂质体中的包被效率几乎没有变化(58-69%)。结果表明,所制备的纳米分散体为粒径在175 ~ 250 nm之间的均匀体系。通过透射电镜研究表明,LA+Carn。脂质体是一种均匀的体系,主要由120-200 nm大小的球形纳米颗粒组成。值得注意的是,在+ 4°和室温下,获得的含有LA和肌肽的脂质体在长期储存(15个月)中是稳定的。结果表明,含有Carn的LA脂质体具有抗氧化作用,可使脂质过氧化产物浓度降低15倍。所获得的脂质体形式对花生四烯酸引起的血小板聚集的影响已被揭示。研究发现,与对照组相比,含有LA和肌肽的脂质体可使血小板聚集程度降低60-70%。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
LIPOSOMAL FORM WITH LIPOIC ACID AND CARNOSINE: PRODUCTION, ANTIPLATELET AND ANTIOXIDANT EFFECT
Optimal conditions were selected for obtaining the liposomal form with lipoic acid (LA) and carnosine. Using methods of active and passive loading, it was possible to achieve high efficiency inclusion of carnosine (60±5%) and lipoic acid (75±5%) in nanoparticles (NPs). It has been shown that the addition of sucrose or cholesterol (Chol) to nanodispersions (NDs) led to a slight decrease in the efficiency incorporation of carnosine in nanoparticles (45±5%). The production of PC-liposomes (PC-Ls) with LA and carnosine by passive loading led to a significant decrease in the efficiency inclusion of carnosine in liposomes (16%). At the same time, the efficiency of inclusion of LA in PC liposomes using methods of both passive and active loading practically did not change (58-69%). It has been found that the obtained nanodispersions are homogeneous system of nanoparticles with size of 175-250 nm. By transmission electron microscopy, it has been shown that LA+Carn. Liposomes represent a homogeneous system consisting mainly of spherical nanoparticles with a size of 120-200 nm. It is important to note that the obtained liposomes with LA and carnosine are stable during long-term storage (15 months) at + 4 ° and at room temperature. It was established that liposomes LA with Carn exhibit an antioxidant effect, leading to a 15-fold decrease in the concentration of lipid peroxidation products. The effect of the obtained liposomal forms on platelet aggregation caused by arachidonic acid has been revealed. It has been found, that liposomes with LA and carnosine reduce the degree of aggregation of platelets by 60-70%, relative to controls.
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