Development of theranostics-type bone-targeted nanodrug carrier for the efficient diagnosis and treatment of bone metastasis

2021 Fiscal Year Final Research Report

• Project/Area Number: 19H04473
• Research Category: Grant-in-Aid for Scientific Research (B)
• Allocation Type: Single-year Grants
• Section: 一般
• Review Section: Basic Section 90120:Biomaterials-related
• Research Institution: Kyoto Pharmaceutical University
• Principal Investigator: Katsumi Hidemasa 京都薬科大学, 薬学部, 准教授 (30434666)
• Co-Investigator(Kenkyū-buntansha): 山本 昌 京都薬科大学, 薬学部, 教授 (00166779) ; 木村 寛之 京都薬科大学, 薬学部, 准教授 (50437240)
• Project Period (FY): 2019-04-01 – 2022-03-31
• Keywords: 薬学 / ドラッグデリバリーシステム / ターゲティング / 骨 / セラノスティクス

Outline of Final Research Achievements

Based on bone targeting technology based on aspartic acid (Asp) modification, we aimed to develop nanoparticles that can efficiently deliver imaging molecules, therapeutic radionuclides and anticancer agents to bone metastases site. By conjugating the hydrophilic group and the hydrophobic group to the terminal group of the Asp-modified branched polymer, we prepared an amphipathic polymer that becomes nanoparticles (micelles) in solution. Anticancer drugs selectively distributed to bone by using Asp-modified nanoparticles after intravenous injection in mice. In tissue distribution imaging by SPECT/CT, bone-selective pharmacokinetics of [111In]Asp-modified nanoparticles were observed. In bone metastasis model mice, administration of anticancer drug-loaded Asp-modified nanoparticles and [90Y] Asp-modified nanoparticles was found to significantly suppress tumor growth in the lower limb bone.

Free Research Field

ドラッグデリバリーシステム

Academic Significance and Societal Importance of the Research Achievements

骨転移は難治性癌性疼痛等の骨関連事象を伴い患者の QOL の低下ひいては死期を早めることから、その診断・治療法の開発が切望される。本研究では、抗癌剤やイメージング用・治療用放射性核種などを効率良く骨へ送達可能な薬物ナノ粒子を開発することに成功した。これらの知見は骨転移診断・治療法の開発に対して有用な情報を提供するものであると考える。