In silico, in vitro, and in vivo methods to analyse drug permeation across the blood-brain barrier: A critical review

Introduction The existence of the blood–brain barrier in the human body leads to the insufficiency in delivering therapeutic compounds into the brain for the effective treatment of various neurological disorders. In order to determine the possibility of such agents to penetrate through the blood–brain barrier, different in silico, in vitro and in vivo methods may be implemented. Some of them are often provided with unreliable results while others are not feasible in high-throughput screening environment. The goal of this review was to characterise the latest state-of-the-art methods that have been developed and used in the pharmaceutical research in the last few decades to assess the permeation of novel therapeutic entities across the blood–brain barrier. We carried out a literature research and study selection by searching for published biomedical articles in the PubMed archive. Conclusion