Intracerebral Diffusion of New Cholesterol-Based Anticancer Conjugate in Tumor-Bearing Rat Model

P u rp o s e:To study the diffusion and affinity in brain of a new cholesterol- based boron anticancer conjugate (cho- lesteryl 1,12-dicarba-closo-dodecaborane 1- carboxylate,BCH) using a tumor- bearing rat model and to examine the stability of BCH in the presence of cho- lesterol esterase and lipoprotein lipase. Methods:The tumor-bearing rat model was produced by intracerebral implanta- tion of rat 9L glioma cells.BCH was for- mulated in liposomes to enhance the aqueous solubility due to its extremely hydrophobic nature.Ten µl of BCH lipo- somes containing 150 µg BCH/mL was administrated to tumor-bearing rats intracerebrally and the BCH concentra- tions in tumor and normal tissues were examined at different time points.The degradation profiles of BCH and the control,cholesterol oleate,in cholesterol