Nanoparticles with surface features of dendritic oligopeptides as potential oral drug delivery systems.

Journal of Materials Chemistry. B, Materials for Biology and Medicine
Yuli BaiYuan Huang

Abstract

Surface features are key to the transcellular transport of nanoparticles (NPs) across intestinal epithelium cells. Endowing the NPs with specific surface features adapted to the physiological conditions of the gastrointestinal (GI) tract holds great potential for the oral delivery of peptide/protein drugs. Therefore, in this work, a glutamic acid conjugated amphiphilic dendrimer (Glu-APD) was synthesized to replace the widely used 1,2-distearoyl-sn-glycero-3-phosphatidyl-ethanolamine-polyethylene glycol (DSPE-PEG) in the preparation of poly(lactic-co-glycolic acid) (PLGA)-based NPs. Glu-APD could provide the formed NPs (Glu-APD NPs) with specific surface features of dendritic oligopeptides. With such surface features, Glu-APD NPs exhibited a 7.78-fold increase in cellular uptake and a 2.17-fold increase in the transepithelial transport amount compared with those of the DSPE-PEG2000 modified counterparts (P NPs). Instead of a dominant clathrin-mediated endocytosis as shown by P NPs, Glu-APD can provide the NPs with optional endocytosis pathways (i.e. clathrin-mediated, caveolae-mediated and micropinocytosis pathways), with the involvement of oligopeptide transporters and amino acid transporters, subsequently leading to a broaden...Continue Reading

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Methods Mentioned

BETA
amidation
nuclear magnetic resonance
dynamic light scattering
transmission electron microscopy
fluorescence microscopy
nanoprecipitation
enzyme-linked immunosorbent assay

Software Mentioned

Drug and Statistics
SPSS
DAS

Related Concepts

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