Drug discovery todayOct 14, 2008

Targeting cancer drugs across the blood-brain barrier using chemical changes or drug nanoparticles

mRNA Technology Weekly Brief ↗PubMed ↗DOI ↗

Updated Apr 4, 2026

Abstract

Efforts to improve drug delivery across the blood-brain barrier (BBB) are focused on chemically modifying drugs and nanoparticles.

The blood-brain barrier poses significant challenges for drug distribution to the central nervous system.
Research is centered on developing chemically modified drugs and nanoparticulate vectors to enhance BBB penetration.
Chemical functionalization of drugs and drug delivery systems is being explored as a strategy to overcome biological barriers.
Endogenous transporters at the BBB may play a role in facilitating drug delivery.

Simplified

One of the most challenging problems, if not the most challenging, in drug development is not to develop drugs to treat diseases of the central nervous system (CNS), but to manage to distribute them to the CNS across the blood-brain barrier (BBB) using transvascular routes following intravenous administration. The development of BBB targeting technologies is a very active field of research and development. One goal is to develop chemically modified derivatives of drugs or chemically modified nanoparticulate vectors of drugs, capable of crossing biological barriers, in particular the BBB. This manuscript will review the approaches that have been explored to achieve these goals, using chemical functionalization of drugs or of drug vector systems and endogenous transporters at the BBB.

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Targeting cancer drugs across the blood-brain barrier using chemical changes or drug nanoparticles

Abstract

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