Cancer and the blood-brain barrier: 'Trojan horses' for courses?

M. Mazza, I. F. Uchegbu, A. G. Schätzlein

    Research output: Contribution to journalArticlepeer-review


    The blood-brain barrier (BBB) limits the bioavailability of most bioactive molecules and drugs in the CNS, leaving clinicians with only a few options for pharmacotherapy. In this issue Regina et al. demonstrate that a 'Trojan horse' drug conjugate, acting as a substrate of a physiological BBB receptor that facilitates transcytosis, significantly improves drug transport into the CNS. Specifically, the low-density lipoprotein receptor-related protein (LRP) is used to carry a conjugate of paclitaxel and Angiopep-2, an aprotinin-derived peptide, across the BBB. Interestingly, in its conjugated form paclitaxel circumvents the efflux pumps at the BBB but still retains its activity against microtubules. Importantly, the authors were able to demonstrate improved therapeutic efficacy of this approach in orthotopic models of primary and metastatic brain cancer. This proof-of-principle study thus represents a milestone for drug delivery across the BBB but also a starting point for studies exploring wider applicability and potential limitations of the approach. © 2008 Macmillan Publishers Limited All rights reserved.
    Original languageEnglish
    Pages (from-to)149-151
    Number of pages2
    JournalBritish Journal of Pharmacology
    Issue number2
    Publication statusPublished - Sept 2008


    • Blood-brain barrier
    • Brain cancer
    • Drug conjugates
    • Drug delivery
    • Low-density lipoprotein receptor-related protein
    • Paclitaxel


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