Development and in vitro characterization of insulin loaded whey protein and alginate microparticles
Development and in vitro characterization of insulin loaded whey protein and alginate microparticles
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DOI：
10.1016/j.ijpharm.2012.10.003
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发表时间：
2012-12-15
影响因子：
5.8
通讯作者：
Beyssac, Eric
中科院分区：
文献类型：
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作者：
Deat-Laine, Emmanuelle;Hoffart, Valerie;Beyssac, Eric
以变性乳清蛋白(WP)和海藻酸盐(ALG)为原料，采用钙离子挤出/冷凝胶法将胰岛素包埋在微粒(MP)中。包封率高达85%。研究了胰岛素对聚合物粘度和微粒行为的影响。胰岛素似乎通过非共价结合和空间位阻与WP链相互作用。这种影响被ALG的添加所平衡。然而，胰岛素在酸性和肠溶出介质中都以扩散的方式迅速释放。尽管体外释放速度很快，但WP/ALG MP对胰蛋白酶和α-胰凝乳酶有重要的酶抑制作用。因此，WP/ALG MP对酶降解具有有效的胰岛素保护作用。上述结果表明，基于WP的微球是一种很有前途的改善胰岛素口服给药的载体。(C)2012爱思唯尔B.V.保留所有权利。
Insulin was encapsulated into microparticles (MP) made of denaturized whey proteins (WP) and alginate (ALG) using an extrusion/cold gelation process with calcium ions. High encapsulation efficiency of 85% was obtained. Influence of insulin on polymeric viscosity and on microparticle behavior was evaluated. Insulin seemed to interact with WP chains by non covalent binding and steric hindrance. This influence was balanced by ALG addition. Nevertheless, insulin was released rapidly by diffusion at both acidic and intestinal dissolution media. Despite this fast in vitro release, WP/ALG MP showed an important enzymatic inhibition effect on trypsin and alpha-chymotrypsin. Thus, WP/ALG MP contributed to an effective insulin protection towards enzymatic degradation. The aforementioned results suggested that WP based microparticles are a promising carrier for improving oral delivery of insulin. (C) 2012 Elsevier B. V. All rights reserved.