Faculty of Pharmacy, Azad University of Medical Sciences, Tehran, Iran.
Nanomedicine. 2010 Feb;6(1):58-63. doi: 10.1016/j.nano.2009.04.007. Epub 2009 May 15.
In the past decade, many strategies have been developed to enhance oral protein delivery. The aim of the current work was to develop a nanoparticulate system based on ionic gelation between chitosan and Arabic gum for loading of insulin. Various formulations were prepared using 2(3) factorial designs. The optimum association efficiency was obtained for formulations F2, F5, and F8. The release profile of insulin in phosphate buffer solutions (pH 6.5 and pH 7.2) is completely different than that in acidic medium (pH 1.2). Increased solubility of chitosan in acidic medium and better swelling of Arabic gum chains at pH >6.5 resulted in lower insulin release of nanoparticles at pH 6.5 in comparison with that of the other pH mediums. The values of the exponent n were 0.49 and 0.82 for formulations F8 and F5, respectively, indicating a non-Fickian transport. This suggests that release is possibly controlled by diffusion or relaxation of the polymer chains.
This paper summarizes the development of a nanoparticulate system based on ionic gelation between chitosan and gum Arabic for oral delivery of insulin. If preclinical studies in animal models will indicate reliable and quantifiable delivery of insulin, this method may pave the way to a novel and less invasive way of administering insulin to diabetes patients.
在过去的十年中,已经开发出许多策略来增强口服蛋白质的传递。目前工作的目的是开发一种基于壳聚糖和阿拉伯胶之间的离子凝胶化的纳米颗粒系统,用于负载胰岛素。使用 2(3) 因子设计制备了各种配方。对于配方 F2、F5 和 F8,获得了最佳的结合效率。胰岛素在磷酸盐缓冲溶液(pH6.5 和 pH7.2)中的释放曲线与在酸性介质(pH1.2)中的释放曲线完全不同。在酸性介质中壳聚糖的溶解度增加和在 pH >6.5 时阿拉伯胶链的更好溶胀导致在 pH6.5 时纳米颗粒中胰岛素的释放低于其他 pH 介质。对于配方 F8 和 F5,指数 n 的值分别为 0.49 和 0.82,表明非菲克扩散。这表明释放可能受扩散或聚合物链的松弛控制。
本文总结了一种基于壳聚糖和阿拉伯胶之间的离子凝胶化的纳米颗粒系统的开发,用于口服传递胰岛素。如果动物模型的临床前研究表明胰岛素的可靠和可量化传递,这种方法可能为糖尿病患者提供一种新颖的、侵入性较小的胰岛素给药方式。