Developments in encapsulation of insulin: Is oral delivery now possible?

A. Singh, Yizhen Guo, Anika Singh, Wenrui Xie, Patrick Jiang
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引用次数: 12

Abstract

This review presents the possibilities of oral delivery of insulin. Insulin, being readily destroyed/ transformed by the proteolytic enzymes and first-pass effects in the digestive system, has mainly been administered through injection, such as intravenous injection and transdermal injection. With developments in the material sciences, appropriate encapsulation methodologies have been developed that could be employed to protect insulin from the digestive effects of the human GI system, and thereby have opened a gateway of research exploring the oral route of insulin delivery. One approach is to incorporate insulin into an emulsion with an appropriate oil-phase, which protects the insulin from degradation. Coating with natural or synthetic polymeric materials, or with lipids, followed by size-reduction to 100-1000 nm is applied as another common approaches of insulin encapsulation. Other approaches like liposomes, nanogels, etc. are also being explored. This review gives a summary of methods of preparation as well as in vitro and in vivo bioavailability of insulin through these methods. It is observed that the oral bioavailability of insulin intake has increased from about 0.1% to about 20% for encapsulated insulin.
胰岛素包封的进展:口服给药现在可行吗?
本文综述了口服给药胰岛素的可能性。胰岛素易被蛋白水解酶破坏/转化,在消化系统中有首过效应,主要通过注射方式给药,如静脉注射和经皮注射。随着材料科学的发展,适当的封装方法已经被开发出来,可以用来保护胰岛素免受人体胃肠道系统的消化影响,从而打开了探索口服胰岛素给药途径的研究大门。一种方法是将胰岛素掺入具有适当油相的乳剂中,以防止胰岛素降解。另一种常用的胰岛素包封方法是采用天然或合成聚合物材料或脂质包封,然后将尺寸缩小到100-1000纳米。其他方法如脂质体、纳米凝胶等也在探索中。本文综述了胰岛素的制备方法及其体外和体内生物利用度。研究发现,胶囊胰岛素的口服生物利用度从约0.1%增加到约20%。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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