Development of High Boron Content Liposomes and Their Promising Antitumor Effect for Neutron Capture Therapy of Cancers

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• 作者：Hayato Koganei ; Manabu Ueno ; Shoji Tachikawa ; Lisa Tasaki ; Hyun Seung Ban ; Minoru Suzuki ; Kouichi Shiraishi ; Kumi Kawano ; Masayuki Yokoyama ; Yoshie Maitani ; Koji Ono ; Hiroyuki Nakamura
• 刊名：Bioconjugate Chemistry
• 出版年：2013
• 出版时间：January 16, 2013
• 年：2013
• 卷：24
• 期：1
• 页码：124-132
• 全文大小：366K
• 年卷期：v.24,no.1(January 16, 2013)
• ISSN：1520-4812

文摘

Mercaptoundecahydrododecaborate (BSH)-encapsulating 10% distearoyl boron lipid (DSBL) liposomes were developed as a boron delivery vehicle for neutron capture therapy. The current approach is unique because the liposome shell itself possesses cytocidal potential in addition to its encapsulated agents. BSH-encapsulating 10% DSBL liposomes have high boron content (B/P ratio: 2.6) that enables us to prepare liposome solution with 5000 ppm boron concentration. BSH-encapsulating 10% DSBL liposomes displayed excellent boron delivery efficacy to tumor: boron concentrations reached 174, 93, and 32 ppm at doses of 50, 30, and 15 mg B/kg, respectively. Magnescope was also encapsulated in the 10% DSBL liposomes and the real-time biodistribution of the Magnescope-encapsulating DSBL liposomes was measured in a living body using MRI. Significant antitumor effect was observed in mice injected with BSH-encapsulating 10% DSBL liposomes even at the dose of 15 mg B/kg; the tumor completely disappeared three weeks after thermal neutron irradiation ((1.5鈥?.8) 脳 10¹² neutrons/cm²). The current results enabled us to reduce the total dose of liposomes to less than one-fifth compared with that of the BSH-encapsulating liposomes without reducing the efficacy of boron neutron capture therapy (BNCT).