Bahman Fatemah, Greish Khaled, Taurin Sebastien
Department of Molecular Medicine, Princess Al-Jawhara Centre for Molecular Medicine, School of Medicine and Medical sciences, Arabian Gulf University, Manama, Bahrain.
Pharm Nanotechnol. 2019;7(2):113-128. doi: 10.2174/2211738507666190321110721.
Diabetes is a group of diseases characterized by hyperglycemia and originating from the deficiency or resistance to insulin, or both. Ultimately, the most effective treatment for patients with diabetes involves subcutaneous injections of insulin. However, this route of administration is often painful and inconvenient, as most patients will have to selfadminister it at least twice a day for the rest of their lives. Also, infection, insulin precipitation, and either lipoatrophy or lipohypertrophy are frequently observed at the site of injection. To date, several alternative routes of insulin administration have been explored, including nasal, pulmonary and oral. Although the delivery of insulin is an ideal route for diabetic patients, several limitations have to be overcome such as the rapid degradation of insulin in gastric fluid and low oral bioavailability. Numerous strategies have been carried out to improve these limited parameters such as the use of enzyme inhibitors, absorption enhancers, mucoadhesive polymers and chemical modification for receptor-mediated absorption. Also, insulin-loaded nanocarriers bypass several physiological barriers. This current review focuses on the various barriers existing in the delivery of insulin through the oral route and the strategies undertaken so far to overcome those obstacles using nanocarriers as a potential vehicle of insulin.
糖尿病是一组以高血糖为特征的疾病，其起因是胰岛素缺乏或抵抗，或两者兼而有之。最终，对糖尿病患者最有效的治疗方法是皮下注射胰岛素。然而，这种给药途径往往既痛苦又不方便，因为大多数患者在余生中每天至少要自行注射两次。此外，在注射部位经常会出现感染、胰岛素沉淀以及脂肪萎缩或脂肪增生。迄今为止，已经探索了几种胰岛素给药的替代途径，包括鼻腔、肺部和口服。尽管口服胰岛素给药对糖尿病患者来说是一种理想途径，但仍有几个限制需要克服，比如胰岛素在胃液中迅速降解以及口服生物利用度低。已经开展了许多策略来改善这些受限参数，例如使用酶抑制剂、吸收促进剂、黏膜黏附聚合物以及进行受体介导吸收的化学修饰。此外，载胰岛素纳米载体可绕过多个生理屏障。本综述重点关注口服胰岛素给药过程中存在的各种障碍，以及迄今为止使用纳米载体作为胰岛素潜在载体来克服这些障碍所采取的策略。
