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局部麻醉药在水相和脂质体相之间的分布。

Distribution of local anesthetics between aqueous and liposome phases.

作者信息

Ruokonen Suvi-Katriina, Duša Filip, Rantamäki Antti H, Robciuc Alexandra, Holma Paula, Holopainen Juha M, Abdel-Rehim Mohamed, Wiedmer Susanne K

机构信息

Department of Chemistry, POB 55, 00014 University of Helsinki, Finland.

Department of Chemistry, POB 55, 00014 University of Helsinki, Finland; Institute of Analytical Chemistry of the CAS, v. v. i., Brno, Czechia.

出版信息

J Chromatogr A. 2017 Jan 6;1479:194-203. doi: 10.1016/j.chroma.2016.12.005. Epub 2016 Dec 3.

DOI:10.1016/j.chroma.2016.12.005
PMID:27955893
Abstract

Liposomes were used as biomimetic models in capillary electrokinetic chromatography (EKC) for the determination of distribution constants (K) of certain local anesthetics and a commonly used preservative. Synthetic liposomes comprised phosphatidylcholine and phosphatidylglycerol phospholipids with and without cholesterol. In addition, ghost liposomes made from red blood cell (RBC) lipid extracts were used as pseudostationary phase to acquire information on how the liposome composition affects the interactions between anesthetics and liposomes. These results were compared with theoretical distribution coefficients at pH 7.4. In addition to 25°C, the distribution constants were determined at 37 and 42°C to simulate physiological conditions. Moreover, the usability of five electroosmotic flow markers in liposome (LEKC) and micellar EKC (MEKC) was studied. LEKC was proven to be a convenient and fast technique for obtaining data about the distribution constants of local anesthetics between liposome and aqueous phase. RBC liposomes can be utilized for more representative model of cellular membranes, and the results indicate that the distribution constants of the anesthetics are greatly dependent on the used liposome composition and the amount of cholesterol, while the effect of temperature on the distribution constants is less significant.

摘要

脂质体被用作毛细管电动色谱(EKC)中的仿生模型,用于测定某些局部麻醉剂和一种常用防腐剂的分配常数(K)。合成脂质体由含胆固醇和不含胆固醇的磷脂酰胆碱和磷脂酰甘油磷脂组成。此外,由红细胞(RBC)脂质提取物制成的空脂质体被用作假固定相,以获取有关脂质体组成如何影响麻醉剂与脂质体之间相互作用的信息。这些结果与pH 7.4时的理论分配系数进行了比较。除了25°C外,还在37°C和42°C下测定分配常数以模拟生理条件。此外,研究了五种电渗流标记物在脂质体电动色谱(LEKC)和胶束电动色谱(MEKC)中的可用性。LEKC被证明是一种方便快捷的技术,可用于获取有关局部麻醉剂在脂质体和水相之间分配常数的数据。红细胞脂质体可用于构建更具代表性的细胞膜模型,结果表明麻醉剂的分配常数在很大程度上取决于所用脂质体的组成和胆固醇的含量,而温度对分配常数的影响较小。

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