Enhancement of oral absorption of biological medicines through co-encapsulation with oligoarginine-linked polymers

2014 Fiscal Year Final Research Report

• Project/Area Number: 25670016
• Research Category: Grant-in-Aid for Challenging Exploratory Research
• Allocation Type: Multi-year Fund
• Research Field: Physical pharmacy
• Research Institution: Setsunan University
• Principal Investigator: SAKUMA Shinji 摂南大学, 薬学部, 教授 (80388644)
• Co-Investigator(Kenkyū-buntansha): KAWAKAMI Kohsaku 物質材料研究機構, 生体機能材料ユニット, 主幹研究員 (00455271)
• Project Period (FY): 2013-04-01 – 2015-03-31
• Keywords: 吸収促進 / バイオ医薬 / オリゴアルギニン / オリゴアルギニン固定化高分子 / エレクトロスプレー / 腸溶性

Outline of Final Research Achievements

There are a couple of problems that should be solved to develop oral formulations of biological medicines: safety of absorption enhancers and a reduction of efficacy of the enhancers through dilution in the gastrointestinal tract. We designed enteric-coated particles containing drugs and absorption enhancers. Electrospray deposition was applied for particle preparation. When both a drug and an absorption enhancer were organic compounds with low molecular weights, absorption-enhancing functions was boosted through their co-encapsulation. This was presumably because the drug was always accompanied by the enhancer during the gastrointestinal transit. Oral absorption of insulin was enhanced when it was co-administered with oligoarginine-linked polymers in a solution. When the dosage form was substituted with enteric-coated particles, insulin absorption was considerably reduced. This probably resulted from interactions between formulated substances.

Free Research Field

薬物送達学