Institute of Environment and Sustainable Development in Agriculture, Chinese Academy of Agricultural Sciences, Beijing 100081, China.
Int J Mol Sci. 2022 Mar 20;23(6):3362. doi: 10.3390/ijms23063362.
Diabetes is a chronic metabolic disease characterized by lack of insulin in the body leading to failure of blood glucose regulation. Diabetes patients usually need frequent insulin injections to maintain normal blood glucose levels, which is a painful administration manner. Long-term drug injection brings great physical and psychological burden to diabetic patients. In order to improve the adaptability of patients to use insulin and reduce the pain caused by injection, the development of oral insulin formulations is currently a hot and difficult topic in the field of medicine and pharmacy. Thus, oral insulin delivery is a promising and convenient administration method to relieve the patients. However, insulin as a peptide drug is prone to be degraded by digestive enzymes. In addition, insulin has strong hydrophilicity and large molecular weight and extremely low oral bioavailability. To solve these problems in clinical practice, the oral insulin delivery nanosystems were designed and constructed by rational combination of various nanomaterials and nanotechnology. Such oral nanosystems have the advantages of strong adaptability, small size, convenient processing, long-lasting pharmaceutical activity, and drug controlled-release, so it can effectively improve the oral bioavailability and efficacy of insulin. This review summarizes the basic principles and recent progress in oral delivery nanosystems for insulin, including physiological absorption barrier of oral insulin and the development of materials to nanostructures for oral insulin delivery nanosystems.
糖尿病是一种慢性代谢疾病，其特征是体内缺乏胰岛素，导致血糖调节失败。糖尿病患者通常需要频繁注射胰岛素来维持正常的血糖水平，这种给药方式非常痛苦。长期的药物注射给糖尿病患者带来了巨大的身心负担。为了提高患者对胰岛素的适应性，减少注射带来的疼痛，口服胰岛素制剂的开发目前是医学和药学领域的一个热门和难题。因此，口服胰岛素给药是一种有前途且方便的给药方式，可以缓解患者的痛苦。然而，胰岛素作为一种肽类药物，容易被消化酶降解。此外，胰岛素具有很强的亲水性、大分子量和极低的口服生物利用度。为了解决这些在临床实践中遇到的问题，通过合理组合各种纳米材料和纳米技术，设计并构建了口服胰岛素传递纳米系统。这种口服纳米系统具有适应性强、体积小、加工方便、药物活性持久、药物控释等优点，因此可以有效提高胰岛素的口服生物利用度和疗效。本文综述了胰岛素口服传递纳米系统的基本原理和最新进展，包括口服胰岛素的生理吸收屏障和用于口服胰岛素传递纳米系统的材料向纳米结构的发展。
