Nanocarrier for Oral Peptide Delivery Produced by Polyelectrolyte Complexation in Nanoconfinement

• Published in: Biomacromolecules 2015-08, Vol.16 (8), p.2282-2287
• Main Authors: He, Wei, Parowatkin, Maria, Mailänder, Volker, Flechtner-Mors, Marion, Graf, Robert, Best, Andreas, Koynov, Kaloian, Mohr, Kristin, Ziener, Ulrich, Landfester, Katharina, Crespy, Daniel
• Format: Article
• Language: English
• Subjects: Alginates - chemistry; Chitosan - chemistry; Chitosan - therapeutic use; Drug Carriers; Electrolytes - chemistry; Hexuronic Acids - chemistry; Humans; Hydrophobic and Hydrophilic Interactions; Obesity - drug therapy; Peptide YY - chemistry; Peptide YY - therapeutic use; Polymers - chemistry; Polymers - therapeutic use
• ISSN: 1525-7797; 1526-4602
• DOI: 10.1021/acs.biomac.5b00500

The hydrophilic peptide YY (PYY) is a promising hormone-based antiobesity drug. We present a new concept for the delivery of PYY from pH-responsive chitosan-based nanocarriers. To overcome the drawbacks while retaining the merits of the polyelectrolyte complex (PEC) method, we propose a one-pot approach for the encapsulation of a hydrophilic peptide drug in cross-linked PEC nanocarriers. First, the hydrophilic peptide is encapsulated via polyelectrolyte complexation within water-in-oil miniemulsion droplets. In a second step, the PEC surface is reinforced by controlled interfacial cross-linking. PYY is efficiently encapsulated and released upon pH change. Such nanocarriers are promising candidates for the fight against obesity and, in general, for the oral delivery of protein drugs.