Improvement of oral delivery of hybrid peptide using absorption enhancer

2017 Fiscal Year Final Research Report

• Project/Area Number: 16K18937
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Multi-year Fund
• Research Field: Medical pharmacy
• Research Institution: Mie University (2017); Kyoto University (2016)
• Principal Investigator: Gaowa Arong 三重大学, 医学系研究科, 助教 (50643805)
• Research Collaborator: HORIBE TOMOHISA 京都大学, 大学院医学研究科, 特定准教授 (20467468) ; KOHNO MASAYUKI 京都大学, 大学院医学研究科, 特定講師 (00437203)
• Project Period (FY): 2016-04-01 – 2018-03-31
• Keywords: 薬物動態学 / ペプチド / ドラッグデリバリー / 経口製剤

Outline of Final Research Achievements

The aim of this study was to improve the oral absorption of epidermal growth factor receptor (EGFR)-targeted hybrid peptide (EGFR2R-lytic) using bile acid as an absorption enhancer. The oral formulation of peptide was formed through the electrostatic interaction between the cationic peptide and anionic bile acid. In Caco-2 cell monolayers, absorption permeability of peptide from the peptide formulation was significantly increased compared with that of peptide alone. Furthermore, oral administration of peptide formulation to xenograft nude mouse showed significantly improved anti-tumor activity compared to free peptide. These results suggested that the bile acid is an effective absorption enhancer for improving the oral bioavailability and bioactivity of hybrid peptide.

Free Research Field

医歯薬学