Brain Penetration and Efficacy of Different Mebendazole Polymorphs in a Mouse Brain Tumor Model.

ABSTRACT:

Purpose

Mebendazole (MBZ), first used as an antiparasitic drug, shows preclinical efficacy in models of glioblastoma and medulloblastoma. Three different mebendazole polymorphs (A, B, and C) exist, and a detailed assessment of the brain penetration, pharmacokinetics, and antitumor properties of each individual mebendazole polymorph is necessary to improve mebendazole-based brain cancer therapy.

Experimental design and results

In this study, various marketed and custom-formulated mebendazole tablets were analyzed for their polymorph content by IR spectroscopy and subsequently tested in an orthotopic GL261 mouse glioma model for efficacy and tolerability. The pharmacokinetics and brain concentration of mebendazole polymorphs and two main metabolites were analyzed by LC/MS. We

SUBMITTER: Bai RY 

PROVIDER: S-EPMC4526400 | biostudies-literature | 2015 Aug

REPOSITORIES: biostudies-literature