University of Copenhagen, Faculty of Health and Medical Sciences, Department of Pharmacy, 2100 Copenhagen Ø, Denmark.
Expert Opin Drug Deliv. 2012 Oct;9(10):1289-304. doi: 10.1517/17425247.2012.717068. Epub 2012 Aug 17.
In order to successfully develop lipid-based drug delivery systems (DDS) for oral administration of peptides and proteins, it is important to gain an understanding of the colloid structures formed by these DDS, the mode of peptide and protein incorporation as well as the mechanism by which intestinal absorption of peptides and proteins is promoted.
The present paper reviews the literature on lipid-based DDS, employed for oral delivery of peptides and proteins and highlights the mechanisms by which the different lipid-based carriers are expected to overcome the two most important barriers (extensive enzymatic degradation and poor transmucosal permeability). This paper also gives a clear-cut idea about advantages and drawbacks of using different lipidic colloidal carriers ((micro)emulsions, solid lipid core particles and liposomes) for oral delivery of peptides and proteins.
Lipid-based DDS are safe and suitable for oral delivery of peptides and proteins. Significant progress has been made in this area with several technologies on clinical trials. However, a better understanding of the mechanism of action in vivo is needed in order to improve the design and development of lipid-based DDS with the desired bioavailability and therapeutic profile.
为了成功开发用于肽和蛋白质口服给药的基于脂质的药物传递系统(DDS),了解这些 DDS 形成的胶体结构、肽和蛋白质的掺入方式以及促进肽和蛋白质肠吸收的机制非常重要。
本文综述了用于肽和蛋白质口服给药的基于脂质的 DDS 的文献,并强调了不同基于脂质的载体预期克服两个最重要障碍(广泛的酶降解和较差的跨黏膜通透性)的机制。本文还清楚地介绍了使用不同的脂质胶体载体((微)乳液、固体脂质核颗粒和脂质体)用于肽和蛋白质口服给药的优缺点。
基于脂质的 DDS 安全且适合于肽和蛋白质的口服给药。该领域已取得重大进展,有几种技术正在临床试验中。然而,为了提高基于脂质的 DDS 的设计和开发,使其具有所需的生物利用度和治疗谱,需要更好地了解体内作用机制。