Department of Pharmaceutics, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.
Targeted Drug Delivery Research Center, Pharmaceutical Technology Institute, Mashhad University of Medical Sciences, Mashhad, Iran.
Expert Opin Drug Deliv. 2023 Jul-Dec;20(10):1387-1413. doi: 10.1080/17425247.2023.2266992. Epub 2023 Oct 30.
Diabetes mellitus is one of the challenging health problems worldwide. Multiple daily subcutaneous injection of insulin causes poor compliance in patients. Development of efficient oral formulations to improve the quality of life of such patients has been an important goal in pharmaceutical industry. However, due to serious issues such as low bioavailability and instability, it has not been achieved yet.
Due to functional properties of the vesicles and the fact that hepatic-directed vesicles of insulin could reach the clinical phases, we focused on three main vesicular delivery systems for oral delivery of insulin: liposomes, niosomes, and polymersomes. Recent papers were thoroughly discussed to provide a broad overview of such oral delivery systems.
Although conventional liposomes are unstable in the presence of bile salts, their further modifications such as surface coating could increase their stability in the GI tract. Bilosomes showed good flexibility and stability in GI fluids. Also, niosomes were stable, but they could not induce significant hypoglycemia in animal studies. Although polymersomes were effective, they are expensive and there are some issues about their safety and industrial scale-up. Also, we believe that other modifications such as addition of a targeting agent or surface coating of the vesicles could significantly increase the bioavailability of insulin-loaded vesicles.
糖尿病是全球面临的极具挑战性的健康问题之一。由于需要每日多次皮下注射胰岛素，患者的依从性较差。开发高效的口服制剂以提高此类患者的生活质量一直是制药行业的重要目标。然而，由于生物利用度低和不稳定性等严重问题，这一目标尚未实现。
由于囊泡的功能特性，以及肝靶向囊泡的胰岛素已进入临床阶段，我们专注于三种主要的囊泡递药系统用于胰岛素的口服递送：脂质体、非诺体和聚合物体。本文对近期的相关文献进行了深入讨论，以期提供此类口服递药系统的全面概述。
虽然常规脂质体在胆汁盐存在下不稳定，但进一步的修饰，如表面涂层，可以增加其在胃肠道中的稳定性。双体在胃肠道液体中具有良好的灵活性和稳定性。此外，非诺体稳定，但在动物研究中不能引起显著的低血糖。虽然聚合物体有效，但它们昂贵，并且存在一些关于其安全性和工业放大的问题。此外，我们认为其他修饰，如添加靶向剂或囊泡的表面涂层，可以显著提高胰岛素负载囊泡的生物利用度。
