Anticancer-agent glycoside conjugates incorporated in bio-nanocapsules for hepatocellular carcinoma treatment

2018 Fiscal Year Final Research Report

• Project/Area Number: 16K01392
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Research Field: Biomedical engineering/Biomaterial science and engineering
• Research Institution: Oita University
• Principal Investigator: Shimoda Kei 大分大学, 医学部, 准教授 (40284153)
• Research Collaborator: HAMADA Hiroki
• Project Period (FY): 2016-04-01 – 2019-03-31
• Keywords: バイオナノカプセル / タキソール誘導体 / DDS製剤

Outline of Final Research Achievements

Hepatitis B virus surface antigen L particles (bionanocapsules) have been of use for a convenient drug delivery system. However, this system is not effective for delivering taxol. Taxol is one of the most potent anticancer agents used in the treatment of many kinds of solid tumors such as breast and ovarian cancers. It presents disadvantages such as low water-solubility and toxicity toward normal tissues. The glucoside derivative, 7-glycolyltaxol 2''-O-alpha-D-glucoside, was glycosylated by cyclodextrin glucanotransferase to 7-glycolyltaxol 2''-O-alpha-maltooligosides. The enzymatic hydrolysis of 7-glycolyltaxol 2''-O-alpha-maltooligosides gave 7-glycolyltaxol 2''-O-alpha-maltotrioside as a taxol-prodrug. We developed the new delivery system for taxol-prodrug using hepatitis B virus envelope L particles (bionanocapsules).

Free Research Field

薬物送達システム

Academic Significance and Societal Importance of the Research Achievements

ヒトB型肝炎ウイルス表面抗原L蛋白質が酵母小胞体由来のリポソームに埋め込まれた構造のバイオナノカプセルは、肝細胞へ集積する特性をもつ有用な薬物キャリアであるが、抗癌剤を輸送することが困難な問題がある。本研究では、タキソール等の抗癌剤に、グリコシドを結合させた、タキソール誘導体を開発し、バイオナノカプセルへ封入した、肝癌細胞株に対する高い抗癌作用を持つ、肝細胞癌治療に有効な薬物送達システム製剤を開発した。