The glucose-lowering potential of exenatide delivered orally via goblet cell-targeting nanoparticles.

Abstract:

PURPOSE:Exenatide, a potent insulinotropic agent, can be used for the treatment of non-insulin-dependent diabetes mellitus. However, the need for frequent injections seriously limits its therapeutic utility. The aim of present report was to develop an orally available exenatide formulation using goblet cell-targeting nanoparticles (NPs). METHOD:The exenatide-loaded nanoparticles were prepared with modified chitosan which was conjugated with a goblet cell-target peptide, CSKSSDYQC (CSK) peptide. RESULTS:The CSK-chitosan nanoparticles shown reduced chitosan toxicity and enhanced the permeation of drugs across the Caco-2/HT-29 co-cultured cell monolayer, which simulated the intestinal epithelium. Following the oral administration of near-infrared fluorescent probe Cy-7-loaded NPs to mice, the distribution of the drugs was investigated with a near-infrared in vivo image system (FX Pro, Bruker, USA). The results showed that Cy-7 fluorescence disseminated from the oesophagus, then to stomach and small intestine and then was absorbed into hepatic, finally into the bladder; over time, Cy-7 was metabolized and excreted. The bioavailability of the modified nanoparticles was found to be 1.7-fold higher compared with the unmodified ones, and the hypoglycemic effect was also better. CONCLUSION:CSK peptide-modified chitosan nanoparticles could be a potential therapeutics for Type II diabetes patients.

journal_name

Pharm Res

journal_title

Pharmaceutical research

authors

Li X,Wang C,Liang R,Sun F,Shi Y,Wang A,Liu W,Sun K,Li Y

doi

10.1007/s11095-014-1513-1

subject

Has Abstract

pub_date

2015-03-01 00:00:00

pages

1017-27

issue

3

eissn

0724-8741

issn

1573-904X

journal_volume

32

pub_type

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