Preparation and Characterization of Lys 27-amine Specific PEGylated Exendin-4 (1-39) forImproved Biological Potency via Intranasal Route

摘要

This study is accomplished to increase thenasal permeability and the protrolytic stability ofExendin Exendin-4 by the site site-specific PEGylation technique,and ultimat ultimately to improve in vivo biological efficacyely via intranasal route. Exendin Exendin-4 was prepared by thecondensation reation of Exendin Exendin-4 with either PEG PEG-SMB(MW 1K) or PEG PEG-SPA(MW 1K, 2K) using a0.3% TEA/DMSO solution. Then, PEGylatedExendin Exendin-4s led to the signific significantly increasedantly absorption and proteolytic stability after nasaladministration versus unmodified Exendin Exendin-4.