Influence of bile acids and their derivatives on drug transport into central nervous system

Primary brain tumors as well as central nervous system (CNS) metastases are in focus of clinical and scientific interest because of the complexity of their treatment due to their location behind the blood-brain barrier (BBB). The main obstacle for efficacy of antitumor drugs in treatment of brain tumors is their low penetrance across the BBB and decreased drug delivery to malignant cells. Previously published results of our scientific group show that bile acids (BAs) and their derivatives have impact on improvement of the absorption, bioavailability and pharmacodynamic of several drugs1,2. In addition, current preliminary results of our group provides the evidence supporting the claim that antitumor drugs have the ability to cross the BBB when administered with BAs. That ability can be exploited by taking a part in novel drug carrier designs. BAs represent a drug carrier system as a part of a mixed micelle composition, bilosomes and conjugates with various drugs. Modern strategies addressed to this issue comprize intranasal drug administration, ligand conjugation, BBB disruption and use of BAs and nanomaterials for CNS drug delivery. Our present research discusses the current knowledge related to bile acid molecules as drug penetration modifying agents, with the focus on central nervous system antitumor drug delivery.