Development of a sprayable smart gel preparation with excellent intranasal retention ability of peptide drugs

2019 Fiscal Year Final Research Report

• Project/Area Number: 17K08468
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Medical pharmacy
• Research Institution: Nihon University
• Principal Investigator: HASHIZAKI Kaname 日本大学, 薬学部, 准教授 (60318459)
• Co-Investigator(Kenkyū-buntansha): 藤井 まき子 日本大学, 薬学部, 教授 (50199296) ; 三浦 基文 日本大学, 薬学部, 准教授 (60385979)
• Project Period (FY): 2017-04-01 – 2020-03-31
• Keywords: スマートゲル製剤 / 経鼻投与製剤 / レシチン逆紐状ミセル / リポソーム架橋ゲル / レオロジー

Outline of Final Research Achievements

In recent years, nasal administration has been attracting attention as an alternative administration route to injection. However, it is very difficult to absorb a water-soluble peptide or protein drug having a large molecular weight from the nasal mucosa. The purpose of this research is to develop a nasal absorption preparation that can be administered by spraying using a smart gel composed of supramolecules. As a result, we have succeeded in clarifying the spraying property of the gel consisting of wormlike micelles and developing a new technology for encapsulating a water-soluble polymer in lecithin reverse wormlike micelles. We also succeeded in developing a liposome cross-linked gel as a new formulation base.

Free Research Field

物理化学

Academic Significance and Societal Importance of the Research Achievements

経鼻投与製剤の吸収改善技術に関しては、透過促進剤や酵素阻害剤などを用いた化学的アプローチが多く、基剤の物理化学的な性質と鼻粘膜との関係を考慮した製剤学的アプローチは少ない。我々は、超分子からなるスマートゲル技術に注目し、本来油に溶けない水溶性高分子をオイルゲル中に溶解する技術や新規基剤の開発に成功した。スマートゲルの経鼻投与により、種々のペプチドのほか、遺伝子なども脳内送達が可能になるものと期待され、その意義は非常に大きい。