Blood–brain barrier transporters: a translational consideration for CNS delivery of neurotherapeutics

Ronaldson, Patrick T.; Davis, Thomas P.

doi:10.1080/17425247.2024.2306138

Expert Opinion on Drug Delivery

2024

DOI: 10.1080/17425247.2024.2306138

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Blood–brain barrier transporters: a translational consideration for CNS delivery of neurotherapeutics

Patrick T. Ronaldson,

Thomas P. Davis

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2024

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Cited by 3 publications

References 208 publications

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Brain delivery enabled by transient blood–brain barrier disruption induced by regadenoson: a PET imaging study

Hosten,

Goutal,

Leterrier

et al. 2024

Expert Opinion on Drug Delivery

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Brain delivery enabled by transient blood–brain barrier disruption induced by regadenoson: a PET imaging study

Hosten,

Goutal,

Leterrier

et al. 2024

Expert Opinion on Drug Delivery

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Challenges and opportunities in neurometabolic disease treatment with enzyme delivery

Begley,

Gabathuler,

Pastores

et al. 2024

Expert Opinion on Drug Delivery

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Induction of P-glycoprotein overexpression in brain endothelial cells as a model to study blood-brain barrier efflux transport

Hathcock,

Knight,

Tong

et al. 2024

Front. Drug Deliv.

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The blood-brain barrier (BBB) is comprised of specialized brain endothelial cells (BECs) that contribute to maintaining central nervous system (CNS) homeostasis. BECs possess properties such as an array of multi-drug efflux transporters that eject various drugs and toxins, preventing their entry into the CNS. Together, it is estimated that these efflux transporters can eject up to 98% of known xenobiotic compounds. P-glycoprotein (P-gp) is a promiscuous efflux transporter at the BBB and can efflux up to 90 various substrates, representing a major hurdle in CNS drug delivery for therapeutic interventions. This necessitates the study of P-gp to discover drugs that are non-substrates of P-gp as well as to identify novel P-gp inhibitors. Here we report the generation of P-gp overexpressing BECs under the endogenous promoter control that could be used in the screening of P-gp substrates. These cells could provide utility in the design of drugs or identification of novel inhibitors.

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Blood–brain barrier transporters: a translational consideration for CNS delivery of neurotherapeutics

Cited by 3 publications

References 208 publications

Brain delivery enabled by transient blood–brain barrier disruption induced by regadenoson: a PET imaging study

Brain delivery enabled by transient blood–brain barrier disruption induced by regadenoson: a PET imaging study

Challenges and opportunities in neurometabolic disease treatment with enzyme delivery

Induction of P-glycoprotein overexpression in brain endothelial cells as a model to study blood-brain barrier efflux transport

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