Damgé Christiane, Reis Catarina Pinto, Maincent Philippe
National Institute for Health and Medical Research (INSERM), University Louis Pasteur, Faculty of Medicine, Institute of Physiology, 11, rue Humann, 67000-Strasbourg, France.
Expert Opin Drug Deliv. 2008 Jan;5(1):45-68. doi: 10.1517/17425247.5.1.45.
Since its discovery, insulin remains the major treatment for Type 1 diabetes and many Type 2 diabetic patients, with insulin being administered parenterally. The oral route of insulin delivery, being the most comfortable, would also be the most physiologically advantageous in taking advantage of the portal-hepatic route of absorption. However, insulin is less absorbed by the intestinal mucosa and is rapidly degraded enzymatically in the gastrointestinal tract. Polymeric biodegradable and biocompatible nanoparticles have been developed. These nanoparticles protect insulin against degradation and facilitate the uptake of insulin (associated or not associated to the nanoparticles) through a paracellular or a transcellular pathway. In this review, the physicochemical characteristics of polymer composition, in vitro release kinetics and the biological effects of insulin-loaded nanoparticles in experimental diabetes and healthy animals are discussed.
自发现以来，胰岛素仍然是1型糖尿病以及许多2型糖尿病患者的主要治疗药物，胰岛素通过肠胃外给药。胰岛素的口服给药途径是最舒适的，而且在利用门静脉 - 肝吸收途径方面在生理上也是最具优势的。然而，胰岛素在肠道黏膜中的吸收较少，并且在胃肠道中会被酶迅速降解。已经开发出了可生物降解和生物相容的聚合物纳米颗粒。这些纳米颗粒可保护胰岛素不被降解，并通过细胞旁或跨细胞途径促进胰岛素（与纳米颗粒相关或不相关）的摄取。在这篇综述中，讨论了聚合物组成的物理化学特性、体外释放动力学以及载胰岛素纳米颗粒在实验性糖尿病动物和健康动物中的生物学效应。
