Design and evaluation of rapamycin loading liposome for lung cancer therapy

2018 Fiscal Year Final Research Report

• Project/Area Number: 17K15513
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Multi-year Fund
• Research Field: Medical pharmacy
• Research Institution: Kumamoto University (2018); Gifu Pharmaceutical University (2017)
• Principal Investigator: ONODERA Risako 熊本大学, 薬学部, 特任助教 (60720399)
• Project Period (FY): 2017-04-01 – 2019-03-31
• Keywords: リポソーム / 経肺投与製剤 / 表面電荷

Outline of Final Research Achievements

In the present study, to make an attempt to confer a cancer cell-selectivity or macrophage -selectivity to liposome, we newly prepared various liposome, and evaluated the potential as its novel drug carrier for lung cancer. Negatively charged liposomes gave high stability in BALF. High negatively charged liposomes were useful for uptake into macrophage. Furthermore, rapamycin loaded folate (FA)-modified liposome showed the potent antitumor activity in LL2 cells-bearing mice. In conclusion, the present study demonstrated the potentials of negatively charged liposomes and FA-modified liposomes as a novel anticancer drug carrier for lung cancer therapy.

Free Research Field

製剤学

Academic Significance and Societal Importance of the Research Achievements

現在、肺がん治療において、経肺投与可能かつマクロファージ選択性を有する抗がん剤は上市されていない。本申請課題では、リポソーム表面への電荷の付与および表面修飾を施すことで、肺がん治療を目指した経肺投与可能なリポソーム製剤の開発が可能であることが示唆された。さらに、肺がんモデルマウスにおいて、尾静脈投与と比較して経肺投与の有用性が明らかとなった。これら本研究課題で得られた知見は、リポソームの経肺投与製剤の構築に際し、有用な基礎的資料になるものと考えられる。