Functional Stimuli-Responsive Nanogel-Particles for Oral Peptide Delivery: Preparation, Drug-Release Behaviors and In Vitro Cellular Interaction

摘要

Novel nanogel particles composing of thermosensitive poly(N-isopropylacrylamide) core and pH-sensitive surrounding layer of poly(methacrylic acid) grafted with polyethylene glycol) (CSNPs) were developed as an oral peptide delivery device. The CSNPs exhibited both temperature- and pH-sensitive swelling behaviors, allowing drug-loading by equilibrium partitioning under mild conditions such as low temperature and neutral pH, and pH-dependent controlled-release of vancomycin (a model peptide drug). Additionally, the CSNPs were found to show no cytotoxic effect on the Caco-2 cells and to possess an ability to open the tight junctions of the cell monolayers which is a requisite for enhanced permeation of peptide drug across the small intestine.