β-Cyclodextrin-Grafted Chitosan Enhances Intestinal Drug Absorption and Its Preliminary Mechanism Exploration
β-Cyclodextrin (CD) and chitosan (CS) have attracted great attention due to their unique properties and structures. β-Cyclodextrin-grafted chitosan (CD-CS) has been widely used as a drug carrier to prepare nano-formulations for drug delivery. However, few researches have been conducted to investigat...
Gespeichert in:
Veröffentlicht in: | AAPS PharmSciTech 2022-08, Vol.23 (6), p.221-221, Article 221 |
---|---|
Hauptverfasser: | , , , , , , , , , , , |
Format: | Artikel |
Sprache: | eng |
Schlagworte: | |
Online-Zugang: | Volltext |
Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
Zusammenfassung: | β-Cyclodextrin (CD) and chitosan (CS) have attracted great attention due to their unique properties and structures. β-Cyclodextrin-grafted chitosan (CD-CS) has been widely used as a drug carrier to prepare nano-formulations for drug delivery. However, few researches have been conducted to investigate the effect of CD-CS as an excipient on cellular uptake and intestinal absorption. Herein, Caco-2 cells were used to investigate the influence of CD-CS on cellular uptake. The MTT assay showed that CD-CS was non-toxic to Caco-2 cells in concentrations ranging from 15.62 to 125 μg/mL. Confocal laser microscopy and flow cytometry measurements indicated that the uptake ability of Caco-2 cells was significantly enhanced after being treated with CD-CS at a concentration of 31.25 μg/mL or incubation for 0.5 h, and the uptake enhancement gradually increased with increasing CD-CS concentration and incubation time. The Caco-2 monolayer cell model and the everted intestinal sac method were employed to preliminarily explore the mechanism of the improved intestinal absorption. The results demonstrated that CD-CS might open the tight junctions and enhance the clathrin-dependent endocytosis, macro-pinocytosis, and phagocytosis of the intestinal epithelial cells. Such findings can serve as references and inspiration for the design of absorption enhancers.
Graphical abstract |
---|---|
ISSN: | 1530-9932 1530-9932 |
DOI: | 10.1208/s12249-022-02380-z |