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载胰岛素两亲性中空碳纳米球的制备及其口服给药研究。

Preparation of amphiphilic hollow carbon nanosphere loaded insulin for oral delivery.

机构信息

Department of Biochemistry, Central Leather Research Institute (Council of Scientific and Industrial Research), Adyar, Chennai 600 020, India.

出版信息

Colloids Surf B Biointerfaces. 2013 Mar 1;103:238-43. doi: 10.1016/j.colsurfb.2012.10.043. Epub 2012 Nov 2.

Abstract

Hollow amphiphilic carbon nanosphere loaded insulin with biodegradable polymer coating (ACP) for oral delivery, was developed to overcome intestinal epithelial barriers and protect insulin from photolytic enzymes. ACP was characterized by laser diffraction spectroscopy for size, distribution and shape by using transmission electron microscopy. Drug-carrier compatibility was studied individually by FTIR and CD spectroscopy. Insulin encapsulation efficiency and in vitro release were determined by Bradford protein assay. Anti-diabetic activity of ACP loaded insulin was determined using Wistar diabetic rats. The mean size of ACP was ∼330 nm with poly index value of 1. Insulin encapsulation efficiency was 93.35%. We observed that ACP formulation suppressed insulin release in acidic media and promoted a sustained release at near neutral conditions. Hence, ACP insulin could be an alternative for injections to diabetic patients.

摘要

载有可生物降解聚合物涂层胰岛素的中空两亲性碳纳米球(ACP)用于口服递送,旨在克服肠道上皮屏障并保护胰岛素免受光解酶的破坏。使用激光衍射光谱法通过透射电子显微镜对 ACP 的大小、分布和形状进行了特征描述。通过傅里叶变换红外光谱和圆二色光谱分别研究了药物载体的相容性。通过 Bradford 蛋白测定法确定胰岛素的包封效率和体外释放。用 Wistar 糖尿病大鼠测定载有胰岛素的 ACP 的抗糖尿病活性。ACP 的平均粒径约为 330nm,多分散指数值为 1。胰岛素的包封效率为 93.35%。我们观察到 ACP 制剂在酸性介质中抑制胰岛素释放,并在近中性条件下促进持续释放。因此,ACP 胰岛素可能是糖尿病患者注射的替代物。

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