论文已发表
注册即可获取德孚的最新动态
IF 收录期刊
Authors Li Y, Zhu CY
Received 18 October 2016
Accepted for publication 4 January 2017
Published 28 February 2017 Volume 2017:12 Pages 1673—1684
DOI https://doi.org/10.2147/IJN.S125047
Checked for plagiarism Yes
Review by Single-blind
Peer reviewers approved by Dr Amy Norman
Peer reviewer comments 4
Editor who approved publication: Dr Linlin Sun
Abstract: In oral administration, gastrointestinal physiological environment,
gastrointestinal epithelial cell membranes, and blood circulation are typical
biological barriers to hepatic delivery of ligand-modified nanoparticle drug
delivery systems. To elucidate the mechanism of oral hepatic targeting of
cholic acid receptor-mediated nanoliposomes (LPs) (distearoyl
phosphatidylethanolamine–polyethylene glycol–cholic acid-modified LPs, CA-LPs),
evaluations were performed on colon cancer Caco-2 cell monolayers, liver cancer
HepG2 cells, and a rat intestinal perfusion model. CA-LPs, ~100 nm in diameter,
exhibited sustained-release behavior and had the greatest stability in rat
gastrointestinal fluid and serum for both size and entrapment efficiency.
CA-LPs demonstrated highest transport across Caco-2 cells and highest cellular
uptake by HepG2 cells. The enhanced endocytosis of CA-LPs was found to be
mediated by Na+/taurocholate cotransporting
polypeptide and involved the caveolin-mediated endocytosis pathway. Further, we
used fluorescence resonance energy transfer (FRET) technology to show that the
CA-LPs maintained their structural integrity in part during the transport
across the Caco-2 cell monolayer and uptake by HepG2 cells.
Keywords: DSPE–PEG–cholic acid, nanoliposomes,
hepatic targeting via oral administration, mechanism, FRET