Pancreatic lipase digestion: The forgotten barrier in oral administration of lipid-based delivery systems?

被引:3
|
作者
Zupanc, Ozbej
Kushwah, Varun [1 ]
Paudel, Amrit [1 ,2 ]
机构
[1] Res Ctr Pharmaceut Engn GmbH RCPE, Inffeldgasse 13, A-8010 Graz, Austria
[2] Graz Univ Technol, Inst Proc & Particle Engn, Inffeldgasse 13-3, A-8010 Graz, Austria
关键词
Lipid-based delivery systems; Pancreatic lipase; Lipid digestion; Lipase inhibition; pH stat model; IN-VITRO DIGESTION; WATER-SOLUBLE DRUGS; HORMONE-SENSITIVE LIPASE; MEDIUM-CHAIN GLYCERIDES; RAW RICE PARTICLES; GASTRIC DIGESTION; LIPOLYSIS MODEL; FOOD DIGESTION; GASTROINTESTINAL-TRACT; INTESTINAL-ABSORPTION;
D O I
10.1016/j.jconrel.2023.08.024
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
This review highlights the importance of controlling the digestion process of orally administered lipid-based delivery systems (LBDS) and their performance. Oral LBDS are prone to digestion via pancreatic lipase in the small intestine. Rapid or uncontrolled digestion may cause the loss of delivery system integrity, its structural changes, reduced solubilization capacity and physical stability issues. All these events can lead to uncontrolled drug release from the digested LBDS into the gastrointestinal environment, exposing the incorporated drug to precipitation or degradation by luminal proteases. To prevent this, the digestion rate of orally administered LBDS can be estimated by appropriate choice of the formulation type, excipient combinations and their ratios. In addition, in vitro digestion models like pH-stat are useful tools to evaluate the formulation digestion rate. Controlling digestion can be achieved by conventional lipase inhibitors like orlistat, sterically hindering of lipase adsorption on the delivery system surface with polyethylene glycol (PEG) chains, lipase desorption or saturation of the interface with surfactants as well as formulating LBDS with ester-free excipients. Recent in vivo studies demonstrated that digestion inhibition lead to altered pharmacokinetic profiles, where Cmax and Tmax were reduced in spite of same AUC compared to control or even improved oral bioavailability.
引用
收藏
页码:381 / 395
页数:15
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