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响应面法优化烷基酰胺脂质体条件及其在Caco-2细胞单层模型中的吸收特性

Optimization of Conditions of Alkylamides Liposomes by Response Surface Methodology and the Absorption Characteristics of Liposomes in the Caco-2 Cell Monolayer Model.

作者信息

Wang Rui, Rao Chaolong, Liu Qiuyan, Liu Xiong

机构信息

College of Food Science, Southwest University, Chongqing 400715, China.

State Key Laboratory of Southwestern Chinese Medicine Resources, School of Public Health, Chengdu University of Traditional Chinese Medicine, Chengdu 611137, China.

出版信息

ACS Omega. 2024 Feb 21;9(9):10992-11004. doi: 10.1021/acsomega.4c00074. eCollection 2024 Mar 5.

Abstract

alkylamides, as a numbing substance in has many physiological effects. However, the numbing taste and unstable properties limited its application. This study aimed to optimize the preparation process of alkylamides liposomes by response surface methodology (RSM) and to investigate the absorption characteristics of the liposomes through the Caco-2 cell monolayer model. The process parameters of liposomes were as follows: alkylamides was 15 mg, phospholipid-feedstock ratio was 6.14, phospholipid-cholesterol ratio was 8.51, sodium cholate was 33.80 mg, isopropyl myristate was 29.49 mg, and the theoretical encapsulation efficiency of the prepared liposomes could reach 90.23%. Further, the particle size of the liposomes was 155.47 ± 3.16 nm, and the ζ-potential was -34.11 ± 4.34 mV. Meanwhile, the liposomes could be preserved for 14 days under the condition that the content of alkylamides was less than 2 mg/mL and the preservation temperature was lower than 25 °C. Moreover, the uptake characteristics of the alkylamides liposomes in the Caco-2 cell monolayer model were also investigated. The results showed that the alkylamides liposomes could be taken up and absorbed by Caco-2 cells. Also, the alkylamides liposomes had a better uptake performance than the unembedded alkylamides and conformed to the passive uptake.

摘要

烷基酰胺作为一种中的麻醉物质具有多种生理作用。然而,其麻醉味道和不稳定的性质限制了它的应用。本研究旨在通过响应面法(RSM)优化烷基酰胺脂质体的制备工艺,并通过Caco-2细胞单层模型研究脂质体的吸收特性。脂质体的工艺参数如下:烷基酰胺为15mg,磷脂与原料比为6.14,磷脂与胆固醇比为8.51,胆酸钠为33.80mg,肉豆蔻酸异丙酯为29.49mg,制备的脂质体理论包封率可达90.23%。此外,脂质体的粒径为155.47±3.16nm,ζ电位为-34.11±4.34mV。同时,在烷基酰胺含量小于2mg/mL且保存温度低于25℃的条件下,脂质体可保存14天。此外,还研究了烷基酰胺脂质体在Caco-2细胞单层模型中的摄取特性。结果表明,烷基酰胺脂质体可被Caco-2细胞摄取和吸收。此外,烷基酰胺脂质体的摄取性能优于未包封的烷基酰胺,且符合被动摄取。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d59d/10918836/cd491e2d2694/ao4c00074_0001.jpg

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