Potential use of folate-appended methyl-?-cyclodextrin as an anticancer agent.

ABSTRACT: To obtain a tumor cell-selectivity of methyl-?-cyclodextrin (M-?-CyD), we newly synthesized folate-appended M-?-CyD (FA-M-?-CyD), and evaluated the potential of FA-M-?-CyD as a novel anticancer agent in vitro and in vivo. Potent antitumor activity and cellular association of FA-M-?-CyD were higher than those of M-?-CyD in KB cells, folate receptor (FR)-positive cells. FA-M-?-CyD drastically inhibited the tumor growth after intratumoral or intravenous injection to FR-positive Colon-26 cells-bearing mice. The antitumor activity of FA-M-?-CyD was comparable and superior to that of doxorubicin after both intratumoral and intravenous administrations, respectively, at the same dose, in the tumor-bearing mice. All of the tumor-bearing mice after an intravenous injection of FA-M-?-CyD survived for at least more than 140 days. Importantly, an intravenous administration of FA-M-?-CyD to tumor-bearing mice did not show any significant change in blood chemistry values. These results strongly suggest that FA-M-?-CyD has the potential as a novel anticancer agent.

SUBMITTER: Onodera R 

PROVIDER: S-EPMC3551233 | biostudies-literature | 2013

REPOSITORIES: biostudies-literature