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刺激敏感脂质体释放与自愈模型的新见解。

New insights on the release and self-healing model of stimuli-sensitive liposomes.

作者信息

Zaborova Olga V, Timoshenko Vadim A, Nardin Corinne, Filippov Sergey K

机构信息

Chemistry Department, Moscow State University, Leninskie gory 1-3, Moscow 119991, Russian Federation.

Universite de Pau et des Pays de l'Adour, E2S UPPA, CNRS, IPREM, Pau 64053, France.

出版信息

J Colloid Interface Sci. 2023 Jun 15;640:558-567. doi: 10.1016/j.jcis.2023.02.099. Epub 2023 Feb 26.

Abstract

The mixing of conventional and pH-sensitive lipids was exploited to design novel stimuli-responsive liposomes (fliposomes) that could be used for smart drug delivery. We deeply investigated the structural properties of the fliposomes and revealed the mechanisms that are involved in a membrane transformation during a pH change. From ITC experiments we observed the existence of a slow process that was attributed to lipid layers arrangement with changing pH. Moreover, we determined for the first time the pKa value of the trigger-lipid in an aqueous milieu that is drastically different from the methanol-based values reported previously in the literature. Furthermore, we studied the release kinetics of encapsulated NaCl and proposed a novel model of release that involves the physical fitting parameters that could be extracted from the release curves fitting. We have obtained for the first time, the values of pores self-healing times and were able to trace their evolution with changing pH, temperature, the amount of lipid-trigger.

摘要

利用传统脂质和pH敏感脂质的混合来设计新型刺激响应脂质体(翻转脂质体),可用于智能药物递送。我们深入研究了翻转脂质体的结构特性,并揭示了pH变化过程中膜转变所涉及的机制。通过等温滴定量热实验,我们观察到存在一个缓慢过程,这归因于脂质层随pH变化的排列。此外,我们首次确定了水性环境中触发脂质的pKa值,该值与文献中先前报道的基于甲醇的值有很大不同。此外,我们研究了包封的NaCl的释放动力学,并提出了一种新的释放模型,该模型涉及可从释放曲线拟合中提取的物理拟合参数。我们首次获得了孔自我修复时间的值,并能够追踪其随pH、温度、脂质触发剂用量变化的演变。

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