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. 2012 Feb;33(5):1573-82.
doi: 10.1016/j.biomaterials.2011.10.075. Epub 2011 Nov 16.

Goblet cell-targeting nanoparticles for oral insulin delivery and the influence of mucus on insulin transport

Yun Jin  1 , Yupin Song, Xi Zhu, Dan Zhou, Chunhui Chen, Zhirong Zhang, Yuan Huang
Affiliations

Goblet cell-targeting nanoparticles for oral insulin delivery and the influence of mucus on insulin transport

Yun Jin et al. Biomaterials. 2012 Feb.

Abstract

The present study was to demonstrate the effects of goblet cell-targeting nanoparticles on the oral absorption of insulin in vitro, ex vivo and in vivo, and identify the targeting mechanism as well as the influence of mucus. The insulin loaded nanoparticles were prepared using trimethyl chitosan chloride (TMC) modified with a CSKSSDYQC (CSK) targeting peptide. Compared with unmodified nanoparticles, the CSK peptide modification could facilitate the uptake of nanoparticles in villi, enhance the permeation of drugs across the epithelium, meanwhile, induce a significantly higher internalization of drugs via clathrin and caveolae mediated endocytosis on goblet cell-like HT29-MTX cells. In transport studies across Caco-2/HT29-MTX co-cultured cell monolayer (simulating intestinal epithelium), the CSK peptide modification also showed enhanced transport ability, even if the targeting recognition was partially affected by mucus. Moreover, it was found the existence of mucus was propitious to the transport of insulin from both modified and unmodified nanoparticles. In the pharmacological and pharmacokinetic studies in diabetic rats, the orally administrated CSK peptide modified nanoparticles produced a better hypoglycemic effect with a 1.5-fold higher relative bioavailability compared with unmodified ones. In conclusion, CSK peptide modified TMC nanoparticles showed sufficient effectiveness as goblet cell-targeting nanocarriers for oral delivery of insulin.

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Comment in

  • Oral insulin: déjà vu?
    Rubinstein I. Rubinstein I. Nanomedicine (Lond). 2012 May;7(5):631-2. doi: 10.2217/nnm.12.38. Nanomedicine (Lond). 2012. PMID: 22630147 No abstract available.

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