Research Progress on the Mechanism of Nanoparticles Crossing the Intestinal Epithelial Cell Membrane

Abstract

Improving the stability of drugs in the gastrointestinal tract and their penetration ability in the mucosal layer by implementing a nanoparticle delivery strategy is currently a research focus in the pharmaceutical field. However, for most drugs, nanoparticles failed in enhancing their oral absorption on a large scale (4 folds or above), which hinders their clinical application. Recently, several researchers have proved that the intestinal epithelial cell membrane crossing behaviors of nanoparticles deeply influenced their oral absorption, and relevant reviews were rare. In this paper, we systematically review the behaviors of nanoparticles in the intestinal epithelial cell membrane and mainly focus on their intracellular mechanism. The three key complex intracellular processes of nanoparticles are described: uptake by intestinal epithelial cells on the apical side, intracellular transport and basal side exocytosis. We believe that this review will help scientists understand the in vivo performance of nanoparticles in the intestinal epithelial cell membrane and assist in the design of novel strategies for further improving the bioavailability of nanoparticles.

Research Advances of Lipid Nanoparticles in the Treatment of Colorectal Cancer

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Figure 5 Structure of the intestinal mucosal barrier comprising microbial, chemical, mechanical, and immune barriers, along with the mechanism of NPs across the mechanical barrier. 110 Current uptake mechanisms of NPs across intestinal epithelium include macropinocytosis, clathrin-mediated endocytosis (CME), caveolae-mediated endocytosis (CavME), and clathrin/caveolae-independent endocytosis (CIE). Created with BioRender.com.

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Intestinal Membrane Function in Inflammatory Bowel Disease

“…The transcellular route for small hydrophilic and lipophilic compounds and the paracellular route of ions, water, and larger hydrophilic compounds are relevant routes, considering the physiology of the intestinal epithelium. Other routes include the transporter-mediated influx and efflux of nutrients such as sugars, amino acids, and vitamins, as well as xenobiotics, and the endocytotic route for larger peptides and proteins [ 20 , 21 ]. Changes in membrane permeability have been considered important to understanding the intestinal status of UC and CD patients [ 22 ].…”