Methylated β-cyclodextrin as P-gp modulators for deliverance of doxorubicin across an in vitro model of blood–brain barrier

Co-incubations of various β-cyclodextrins and doxorubicin have been evaluated on an in vitro model of blood–brain barrier in order to increase the delivery of this P-gp substrate to the brain. Among these cyclodextrins used, the Rame-β-cyclodextrin and Crysme-β-cyclodextrin increased the transport by a factor of 2 and 3.7, respectively. This increase was attributed to the cholesterol extraction property of these cyclodextrins from brain capillary endothelial cells leading to a modulation of the P-gp activity.