A novel ligand conjugated nanoparticles for oral insulin delivery.

Abstract:

:In order to enhance the interaction between nanocarrier and gastrointestinal epithelial cells, we developed nanoparticles (NPs) modified with targeting ligand FQSIYPpIK (FQS), which specifically interact with integrin αvβ3 receptor expressing on the intestinal epithelium. The targeting NPs were prepared by coating the insulin-loaded poly(lactide-co-glycolide)-monomethoxy-poly(polyethylene glycol) micelle cores with FQS modified trimethyl chitosan chloride. In in vitro study, the fabricated NPs showed ameliorated drug release profile and improved enzymatic stability compared with micelles alone. In the integrin αvβ3 receptor over-expressed Caco-2 cells model, FQS modified NPs exhibited significantly accelerated intracellular uptake due to the active ligand-receptor mediation. Meanwhile, the targeting NPs also showed enhanced transport across the Caco-2 monolayer cells via both transcellular and paracellular pathways. Besides, orally administered FQS modified NPs produced a prominent hypoglycemic response and an increase of the serum insulin concentration in diabetic rats. Both in vitro and in vivo results demonstrated the FQS peptide modified NPs as promising intestinal cell-targeting nanocarriers for efficient oral delivery of insulin.

journal_name

Drug Deliv

journal_title

Drug delivery

authors

Liu C,Shan W,Liu M,Zhu X,Xu J,Xu Y,Huang Y

doi

10.3109/10717544.2015.1058433

subject

Has Abstract

pub_date

2016-07-01 00:00:00

pages

2015-25

issue

6

eissn

1071-7544

issn

1521-0464

journal_volume

23

pub_type

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