Laboratory of Food Chemistry and Nutrition Science, Institute of Food Science and Technology, Chinese Academy of Agricultural Sciences, Key Laboratory of Agro-Products Processing, Ministry of Agriculture and Rural Affairs, No. 2 Yuan Ming Yuan West Road, Haidian District, P.O. Box 5109, Beijing 100193, China.
Laboratory of Food Chemistry and Nutrition Science, Institute of Food Science and Technology, Chinese Academy of Agricultural Sciences, Key Laboratory of Agro-Products Processing, Ministry of Agriculture and Rural Affairs, No. 2 Yuan Ming Yuan West Road, Haidian District, P.O. Box 5109, Beijing 100193, China.
Carbohydr Polym. 2024 Jan 1;323:121364. doi: 10.1016/j.carbpol.2023.121364. Epub 2023 Sep 9.
Diabetes mellitus is a chronic metabolic disease that affects >500 million patients worldwide. Subcutaneous injection of insulin is the most effective treatment at present. However, regular needle injections will cause pain, inflammation, and other adverse consequences. In recent years, significant progress has been made in non-injectable insulin preparations. Oral administration is the best way of administration due to its simplicity, convenience, and good patient compliance. However, oral insulin delivery is hindered by many physiological barriers in the gastrointestinal tract, resulting in the low relative bioavailability of direct oral insulin delivery. To improve the relative bioavailability, a variety of insulin delivery vectors have been developed. Polysaccharides are used to achieve safe and effective insulin loading due to their excellent biocompatibility and protein affinity. The functional characteristics of polysaccharide-based delivery carriers, such as pH responsiveness, mucosal adhesion, and further functionalization modifications, enhance the gastrointestinal absorption and bioavailability of insulin. This paper reviews the materials and structures of oral insulin polysaccharide-based carriers, providing ideas for further improving the relative bioavailability of oral insulin.
糖尿病是一种全球性的慢性代谢疾病,影响着全球超过 5 亿名患者。目前,皮下注射胰岛素是最有效的治疗方法。然而,定期的针剂注射会引起疼痛、炎症等不良反应。近年来,非注射用胰岛素制剂取得了重大进展。口服给药因其简便、方便和良好的患者依从性而成为最佳给药途径。然而,口服胰岛素输送受到胃肠道内多种生理屏障的阻碍,导致直接口服胰岛素输送的相对生物利用度较低。为了提高相对生物利用度,已经开发了多种胰岛素输送载体。多糖由于其优异的生物相容性和蛋白质亲和力,被用于实现安全有效的胰岛素负载。基于多糖的输送载体的功能特性,如 pH 响应性、黏膜黏附性和进一步的功能化修饰,增强了胰岛素的胃肠道吸收和生物利用度。本文综述了口服胰岛素多糖载体的材料和结构,为进一步提高口服胰岛素的相对生物利用度提供了思路。