The DOI matches its OpenAlex record; 35 of the 35 references it cites were found in a registry or an index.
Transport of paclitaxel (Taxol) across the blood-brain barrier in vitro and in vivo
Open accessAbstract
Paclitaxel concentrations in the brain are very low after intravenous injection. Since paclitaxel is excluded from some tumors by p-glycoprotein (p-gp), the same mechanism may prevent entry into the brain. In vitro, paclitaxel transport was examined in capillaries from rat brains by confocal microscopy using BODIPY Fl-paclitaxel. Western blots and immunostaining demonstrated apical expression of p-gp in isolated endothelial cells, vessels, and tissue. Secretion of BODIPY Fl-paclitaxel into capillary lumens was specific and energy-dependent. Steady state luminal fluorescence significantly exceeded cellular fluorescence and was reduced by NaCN, paclitaxel, and SDZ PSC-833 (valspodar), a p-gp blocker. Leukotriene C(4) (LTC(4)), an Mrp2-substrate, had no effect. Luminal accumulation of NBDL-cyclosporin, a p-gp substrate, was inhibited by paclitaxel. In vivo, paclitaxel levels in the brain, liver, kidney, and plasma of nude mice were determined after intravenous injection. Co-administration of valspodar led to increased paclitaxel levels in brains compared to monotherapy. Therapeutic relevance was proven for nude mice with implanted intracerebral human U-118 MG glioblastoma. Whereas paclitaxel did not affect tumor volume, co-administration of paclitaxel (intravenous) and PSC833 (peroral) reduced tumor volume by 90%. Thus, p-gp is an important obstacle preventing paclitaxel entry into the brain, and inhibition of this transporter allows the drug to reach sensitive tumors within the CNS.
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The Blood-Brain Barrier and Cancer: Transporters, Treatment, and Trojan Horses
Deeken, J. F., & Löscher, W. (2007) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-06-2854 · Cited by 721
Advances in tau-focused drug discovery for Alzheimer's disease and related tauopathies
Brunden, K. R., Trojanowski, J. Q., & Lee, V. M.-Y. (2009) · Nature Reviews Drug Discovery · doi:10.1038/nrd2959 · Cited by 440
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Breedveld, P., Beijnen, J. H., & Schellens, J. H. M. (2006) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2005.11.009 · Cited by 323
Metadata
- Authors
- Fellner, S., Bauer, B., Miller, D. S., Schaffrik, M., Fankhänel, M., Spruß, T., Bernhardt, G., Graeff, C., Färber, L., Gschaidmeier, H., Buschauer, A., & Fricker, G.
- Venue
- Journal of Clinical Investigation
- Publisher
- American Society for Clinical Investigation
- Published
- 2002-11-01
- Volume
- 110
- Issue
- 9
- Pages
- 1309-1318
- ISSN
- 0021-9738 (ISSN-L)
- OpenAlex
- W2162592548
- Cited by
- 359
- References
- 35
- FWCI
- 5.90
- Type
- journal article
- Language
- en
- Open access
- green
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- CoChat. (2026). Citation check: Transport of paclitaxel (Taxol) across the blood-brain barrier in vitro and in vivo. https://app.cochat.ai/papers/10.1172/jci15451
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- Fellner, S., Bauer, B., Miller, D. S., Schaffrik, M., Fankhänel, M., Spruß, T., Bernhardt, G., Graeff, C., Färber, L., Gschaidmeier, H., Buschauer, A., & Fricker, G. (2002). Transport of paclitaxel (Taxol) across the blood-brain barrier in vitro and in vivo. Journal of Clinical Investigation. https://doi.org/10.1172/jci15451
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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