Peptide-vector strategy bypasses P-glycoprotein efflux, and enhances brain transport and solubility of paclitaxel

Blanc, E.; Bonnafous, C.; Merida, P.; Cisternino, S.; Clair, P.; Scherrmann, J. M.; Temsamani, J.

Anticancer Drugs

2004-11 / vol 15 / pages 947-54


We present the results obtained with paclitaxel coupled to a peptide-vector SynB3 (PAX-OSUC-SynB3), showing that this peptide-vector enhances the solubility of paclitaxel and its brain uptake in mice using the in situ brain perfusion model. We also show by the in situ brain perfusion in P-glycoprotein (P-gp)-deficient and wild-type mice that vectorized paclitaxel bypasses the P-gp present at the luminal side of the blood-brain barrier. The effect of the vectorized paclitaxel on various cancer cells was not significantly different from that of free paclitaxel. These results indicate that vectorization of paclitaxel may have significant potential for the treatment of brain tumors.

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Cell Line, Tumor; Humans; Animals; Mice; Rats; Biological Transport; Solubility; Cell Cycle/drug effects; Drug Carriers; Antineoplastic Agents, Phytogenic/administration &; Blood-Brain Barrier/*metabolism; dosage/chemistry/*pharmacokinetics; Oligopeptides/*chemistry; P-Glycoprotein/*metabolism; Paclitaxel/administration & dosage/chemistry/*pharmacokinetics; Succinic Acid/chemistry

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