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O-羧甲基壳聚糖-阿拉伯胶凝聚层的肠道靶向递送效能:凝聚酸度的影响及可能机制

Intestine-targeted delivery potency of the O-carboxymethyl chitosan-gum Arabic coacervate: Effects of coacervation acidity and possible mechanism.

作者信息

Huang Guo-Qing, Liu Li-Na, Han Xiao-Na, Xiao Jun-Xia

机构信息

College of Food Science and Engineering, Qingdao Agricultural University, Qingdao 266109, China.

Institute of Agro-Food Science and Technology, Shandong Academy of Agricultural Sciences, Jinan 250100, China.

出版信息

Mater Sci Eng C Mater Biol Appl. 2017 Oct 1;79:423-429. doi: 10.1016/j.msec.2017.05.074. Epub 2017 May 13.

Abstract

The potential of the glutaraldehyde-crosslinked O-carboxymethyl chitosan (O-CMC)-gum Arabic (GA) coacervate as an intestine-targeted delivery system for hydrophobic compounds was concerned. OCMC-GA coacervates and emulsified bovine serum albumin (BSA)-loaded microcapsules were prepared in pH3.0, 4.5, and 6.0 and their swelling behaviors as well as BSA release profiles in simulated gastrointestinal fluids were measured. All the coacervates showed higher swelling ratios in the simulated gastric solution than in the simulated intestine and colon solutions and the values increased as the coacervation pH increased from 3.0 to 6.0, but a reversed trend was observed for the BSA release profile. SEM, TEM, and CLSM analysis revealed that the coacervation acidity influenced the swelling and BSA release behavior by changing the matrix density and O-CMC content of the coacervates. It was concluded that the O-CMC-GA coacervate could be used to deliver hydrophobic compounds to the intestine and its delivery performance could be tailored by selecting appropriate coacervation acidity and crosslinking degree.

摘要

戊二醛交联的O-羧甲基壳聚糖(O-CMC)-阿拉伯胶(GA)凝聚层作为疏水性化合物肠道靶向递送系统的潜力受到关注。在pH3.0、4.5和6.0条件下制备了OCMC-GA凝聚层和负载乳化牛血清白蛋白(BSA)的微胶囊,并测定了它们在模拟胃肠液中的溶胀行为以及BSA释放曲线。所有凝聚层在模拟胃液中的溶胀率均高于模拟肠液和结肠液,且随着凝聚pH值从3.0增加到6.0,溶胀率值升高,但BSA释放曲线呈现相反趋势。扫描电子显微镜(SEM)、透射电子显微镜(TEM)和共聚焦激光扫描显微镜(CLSM)分析表明,凝聚酸度通过改变凝聚层的基质密度和O-CMC含量来影响溶胀和BSA释放行为。得出结论,O-CMC-GA凝聚层可用于将疏水性化合物递送至肠道,并且可以通过选择合适的凝聚酸度和交联度来调整其递送性能。

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