Affiliation:
1. School of Pharmacy, Xi’an Jiaotong University , Xi’an , China
Abstract
Abstract
Objectives
This study focuses on investigating the potential impact of DSPE-PEG polymers on intestinal absorption and related mechanism of berberine in rats.
Methods
Effect of DSPE-PEG polymer on intestinal absorption of berberine was investigated with an in situ closed-loop method in rats. To confirm the safety of DSPE-PEG polymer, morphological observation of rat intestine and measurement of biological markers in the intestinal perfusion of rats was performed. Underling mechanism behind promoting action of DSPE-PEG polymer was explored from its impact on the P-gp function and tight junction using in vitro diffusion chamber system, Caco-2 monolayer cells and western blot.
Key findings
DSPE-PEG polymer demonstrated significant enhancement action on the berberine absorption in rats without any obvious membrane toxicity. DSPE-PEG polymer (1.0%, w/v) induced the most significant promoting effect on berberine absorption specifically in the small intestine of rats. Results of mechanistic studies revealed that DSPE-PEG polymer might not regulate intestinal P-gp function, but significantly down-regulated the expression of tight junction-related proteins, which accordingly led to loosening the tight junctions of intestinal epithelium cells, and consequently increased paracellular absorption of berberine in rats.
Conclusions
DSPE-PEG polymer, as an excellent absorption enhancer, seems very promising in increasing oral bioavailability of berberine.
Funder
National Natural Science Foundation of China
Shannxi Provincial Natural Science
Publisher
Oxford University Press (OUP)
Subject
Pharmaceutical Science,Pharmacology
Cited by
3 articles.
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