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构建双重响应改性瓜尔胶纳米粒子及其在口服胰岛素给药中的应用。

Construction of a double-responsive modified guar gum nanoparticles and its application in oral insulin administration.

机构信息

School of Life Science, South China Normal University, Guangzhou 510631, China.

School of Life Science, South China Normal University, Guangzhou 510631, China; Guangzhou Key Laboratory of Spectral Analysis and Functional Probes, College of Biophotonics, South China Normal University, Guangzhou 510631, China; South China Normal University-Panyu Central Hospital Joint Laboratory of Translational Medical Research, Panyu Central Hospital, Guangzhou 510631, China.

出版信息

Colloids Surf B Biointerfaces. 2022 Dec;220:112858. doi: 10.1016/j.colsurfb.2022.112858. Epub 2022 Sep 22.

DOI:10.1016/j.colsurfb.2022.112858
PMID:36174491
Abstract

The use of intelligent insulin delivery systems has become more important for treating diabetes. In this study, a dual-responsive oral insulin delivery nanocarrier that responds to glucose and pH has been developed. First, the oleic acid hydrophobic modified guar gum (GG) was synthesized by the esterification reaction, and the γ-polyglutamic acid (γ-PGA) was coupled with GG by the amidation reaction. The obtained pH-responsive copolymer (γ-PGA-GG) was cross-linked by concanavalin A to obtain pH/glucose dual-responsive nanocarriers, and insulin was effectively loaded into the dual-responsive nanocarriers. The insulin-loaded nanoparticles can achieve effective pH and glucose responses, releasing insulin on demand. In vitro and in vivo studies demonstrated the dual-responsive nanoparticles can protect insulin against the pH changes in the digestive tract and deliver insulin into the body to exert a hypoglycemic effect. Moreover, the dual-responsive nanoparticles have significant potential to be employed for oral insulin delivery.

摘要

智能胰岛素输送系统在糖尿病治疗中的应用变得越来越重要。在这项研究中,开发了一种对葡萄糖和 pH 值均有响应的双响应口服胰岛素递药纳米载体。首先,通过酯化反应合成了油酸疏水改性瓜尔胶(GG),并通过酰胺化反应将γ-聚谷氨酸(γ-PGA)与 GG 偶联。所得 pH 响应性共聚物(γ-PGA-GG)通过刀豆球蛋白 A 交联得到 pH/葡萄糖双响应纳米载体,胰岛素被有效装载到双响应纳米载体中。载胰岛素的纳米颗粒可以实现有效的 pH 和葡萄糖响应,按需释放胰岛素。体外和体内研究表明,双响应纳米颗粒可以保护胰岛素免受消化道 pH 值变化的影响,并将胰岛素递送到体内发挥降血糖作用。此外,双响应纳米颗粒具有很大的潜力用于口服胰岛素给药。

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