作者：Chao Zheng, Xinge Zhang*, Qianqian, Guo, Chaoxing Li, Zhengpu Zhang*
关键字：nasal delivery, nanoparticles
论文来源：期刊
具体来源：European Journal of Pharmaceutical Science, 2013, in press.
发表时间：2013年

The application of proteins and peptides is hampered by their rapid clearance in liver and other body tissues by proteolytic enzymes, so they are difficult to administer except by the injection. To explore phenylboronic acid-functionalized glycopolymeric nanoparticles as effective carriers for the nasal delivery of proteins and peptides, a novel amphiphilic glycopolymer poly(2-lactobionamidoethyl methacrylate-random-3-acrylamidophenylboronic acid) (p(LAMA-r-AAPBA)) was prepared. p(LAMA-r-AAPBA) could assemble into the nanoparticles with narrow size distribution. Insulin, as a model drug, was efficiently encapsulated within the nanoparticles, and loading capacity was up to 12%. The in vitro study revealed that the release of insulin could be controlled by modifying the composition of glycopolymers. Cell viability showed that p(LAMA-r-AAPBA) nanoparticles had good cytocompatibility. Moreover, the mechanism of nanoparticle internalization into Calu-3 cells was a combination mechanism of clathrin-mediated endocytosis and lipid raft/caveolae-mediated endocytosis. Importantly, there was a significant decrease in the blood glucose levels after the nasal administration of p(LAMA-r-AAPBA) nanoparticles to diabetic rats. Therefore, p(LAMA-r-AAPBA) glycopolymers have a potential application for nasal delivery of proteins and peptides.