Strategic formulization of nobiletin to improve its biopharmaceutical properties for COPD treatment

2018 Fiscal Year Final Research Report

• Project/Area Number: 16K18950
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Multi-year Fund
• Research Field: Medical pharmacy
• Research Institution: University of Shizuoka
• Principal Investigator: Sato Hideyuki 静岡県立大学, 薬学部, 講師 (70739242)
• Project Period (FY): 2016-04-01 – 2019-03-31
• Keywords: 難水溶性化合物 / Nobiletin / 溶解性改善 / 粉末吸入製剤 / 慢性閉塞性肺疾患

Outline of Final Research Achievements

The aim of the present study is to develop novel inhalable formulation of Nobiletin (NOB) for the treatment of chronic obstructive pulmonary disease (COPD). NOB has been known as one of poorly water-soluble polyphenols isolated from citrus peel, which has anti-inflammatory effect, anti-oxidation, inhibition of fibrosis, and anti-apoptotic effect. These beneficial effects might contribute to treat COPD symptoms. Thus, to clarify the applicability of NOB to the treatment of COPD, various kinds of solubilization technologies were applied for developing NOB formulations. We successfully developed solubilized formulation to improve the biopharmaceutical properties of NOB, and a formulization technology to prepare inhalable formulation of poorly water-soluble materials.

Free Research Field

薬剤学，薬物動態学

Academic Significance and Societal Importance of the Research Achievements

慢性閉塞性肺疾患(COPD) の患者数は今後爆発的に増加し，WHO の試算によると2020 年までに世界第3 位の死亡原因になると予想されているにも関わらず，現在のCOPD の診断率は低く，適切な診断・治療が普遍的に実施されていない．また柑橘類由来ポリフェノールであるノビレチン (NOB) は COPD 治療に対するポテンシャルを有するものの，難水溶性をはじめとする物性の悪さのために COPD に対する応用研究がほとんどなされていない．本検討では，NOB を効果的に治療用するための製剤化研究とその剤形開発を戦略的に実行し，これら技術の有用性を明らかとすることに成功した．