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将大花田菁提取物包裹于聚合物胶束中以提高其溶解度、稳定性及抗菌活性。

Encapsulation of Sesbania grandiflora extract in polymeric micelles to enhance its solubility, stability, and antibacterial activity.

作者信息

Anantaworasakul Pimporn, Okonogi Siriporn

机构信息

a Department of Pharmaceutical Sciences, Faculty of Pharmacy , Chiang Mai University , Chiang Mai , Thailand.

出版信息

J Microencapsul. 2017 Feb;34(1):73-81. doi: 10.1080/02652048.2017.1284277. Epub 2017 Feb 5.

Abstract

Clinical applications of Sesbania grandiflora bark extract (SGE) are limited because of its poor water solubility and stability. SGE was loaded in micelles of Pluronics. In vitro and in vivo antibacterial and toxicity tests were investigated using broth dilution and silkworm model. Aqueous solubility of SGE was improved by these micelles. Activity and toxicity of SGE loaded micelles were dependent on type and concentration of Pluronics. The micelles composed of 1:3 SGE to Pluronic F68 (SGE-PF68-13) showed small size (24.95 ± 0.34 nm), narrow PdI (<0.2), high entrapment efficiency (99.63 ± 0.19%) and negative zeta potential (-41.53 ± 0.15 mV). Stability of SGE in SGE-PF68-13 was 10 times higher than the unentrapped SGE. SGE-PF68-13 showed a dose dependent activity and significantly higher therapeutic effect than the unentrapped SGE. It is concluded that encapsulation of SGE in Pluronic micelles can enhance SGE solubility, stability, and antibacterial activity. SGE-PF68-13 is suitable for further study in mammalian animals.

摘要

大花田菁树皮提取物(SGE)因其较差的水溶性和稳定性,临床应用受到限制。SGE被载入普朗尼克胶束中。采用肉汤稀释法和家蚕模型进行体外和体内抗菌及毒性试验。这些胶束提高了SGE的水溶性。载入SGE的胶束的活性和毒性取决于普朗尼克的类型和浓度。由SGE与普朗尼克F68按1:3组成的胶束(SGE-PF68-13)粒径小(24.95±0.34nm)、分散度指数窄(<0.2)、包封率高(99.63±0.19%)且zeta电位为负(-41.53±0.15mV)。SGE在SGE-PF68-13中的稳定性比未包封的SGE高10倍。SGE-PF68-13表现出剂量依赖性活性,且治疗效果显著高于未包封的SGE。得出结论:将SGE包封于普朗尼克胶束中可提高SGE的溶解度、稳定性和抗菌活性。SGE-PF68-13适合在哺乳动物中进一步研究。

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