| 赖氨酸在甘草次酸弹性囊泡形成过程中的作用机制 |
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| 引用本文： | 李爽,邱玉琴,张锁慧,高云华.赖氨酸在甘草次酸弹性囊泡形成过程中的作用机制[J].物理化学学报,2011,27(9):2167-2172. |
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| 作者姓名： | 李爽 邱玉琴 张锁慧 高云华 |
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| 作者单位： | 1. Key Laboratory of Photochemical Conversion and Optoelectronic Materials, Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Beijing 100190, P. R. China;
2. Graduate University of Chinese Academy of Sciences, Beijing 100049, P. R. China |
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| 摘 要： | 制备和评价含赖氨酸的甘草次酸弹性囊泡, 并考察赖氨酸在囊泡形成过程中的作用机制. 在水合介质中加入赖氨酸, 利用薄膜-高压均质法制备甘草次酸弹性囊泡. 并合成了甘草次酸赖氨酸盐及其弹性囊泡作为对比制剂. 通过对粒径、zeta电位、包封率、相转变温度、变形性和体外经皮渗透性的测试, 考察赖氨酸在甘草次酸弹性囊泡中的存在形式及作用. 结果显示加入赖氨酸后, 甘草次酸弹性囊泡的粒径略有降低, 膜相转变温度降低, 包封率和囊泡变形性显著提高, 载药量提高近30倍(1.5 mg·mL-1), 并显著高于其赖氨酸盐所形成囊泡的载药量和弹性. 此外, 赖氨酸的加入使弹性囊泡的变形能力增加, 8 h累积透过量和皮肤驻留量分别提高4.3倍和9.2倍. 表明赖氨酸与甘草次酸形成离子缔合物, 促进甘草次酸参与膜的形成, 使膜的流动性增加, 赖氨酸与弹性囊泡对提高囊泡载药量起协同作用.
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| 关 键 词： | 甘草次酸 弹性囊泡 赖氨酸 载药量 机理 |
| 收稿时间： | 2011-05-17 |
Mechanism of Lysine on the Formation of Glycyrrhetic Acid Elastic Vesicles |
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| LI Shuang,QIU Yu-Qin,ZHANG Suo-Hui,GAO Yun-Hua.Mechanism of Lysine on the Formation of Glycyrrhetic Acid Elastic Vesicles[J].Acta Physico-Chimica Sinica,2011,27(9):2167-2172. |
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| Authors: | LI Shuang QIU Yu-Qin ZHANG Suo-Hui GAO Yun-Hua |
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| Institution: | 1. Key Laboratory of Photochemical Conversion and Optoelectronic Materials, Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Beijing 100190, P. R. China;
2. Graduate University of Chinese Academy of Sciences, Beijing 100049, P. R. China |
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| Abstract: | Elastic vesicles of glycyrrhetic acid(GA) with lysine in the aqueous phase were prepared by the film-high pressure homogenization method.The influence of lysine on the formation of GA elastic vesicles was evaluated in this work.The lysine salt of GA was synthesized and entrapped in elastic vesicles as a control formulation.The particle size,zeta-potential,entrapment efficiency,phase transformation temperature,deformability of the elastic vesicles,and the permeation of GA through rat skin were investigated.B... |
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| Keywords: | Glycyrrhetic acid Elastic vesicle Lysine Drug-loading Mechanism |
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