Folate-appended cyclodextrin improves the intratumoral accumulation of existing boron compounds

Authors:   Matsumoto Y., Hattori K., Arima H., Motoyama K., Higashi T., Ishikawa H., Fukumitsu N., Aihara T., Nakai K., Kumada H., Sakurai H.
Journal: Applied Radiation and Isotopes
https://doi.org/10.1016/j.apradiso.2020.109201
Abstract: In this study, the tumor accumulation and antitumor effect of folate-modified cyclodextrin (ND201) purified with folate receptor (FR) connotated with BSH were examined. ND201 and BSH were stably bound in blood, and the mixing ratio 1:1 was most efficient. ND-BSH showed higher boron concentration (38.5 ppm) than BSH alone (11.25 ppm). The maximum ND-BSH tumor/blood ratio was also markedly higher (6.58) than that of BSH alone (1.04). ND-BSH showed a significant antitumor effect compared with BSH after neutron irradiation.