• DOI:10.1007/s11095-006-0022-2
• Corpus ID: 231917

Enhanced Oral Paclitaxel Bioavailability After Administration of Paclitaxel-Loaded Lipid Nanocapsules

@article{Peltier2006EnhancedOP,
  title={Enhanced Oral Paclitaxel Bioavailability After Administration of Paclitaxel-Loaded Lipid Nanocapsules},
  author={S. Peltier and J M Oger and Fr{\'e}d{\'e}ric Lagarce and William Couet and Jean Pierre Benoit},
  journal={Pharmaceutical Research},
  year={2006},
  volume={23},
  pages={1243-1250}
}

• S. Peltier, J. Oger, +2 authors J. Benoit
• Published 25 May 2006
• Chemistry, Biology, Medicine
• Pharmaceutical Research

PurposeThe aim of this study was to evaluate the pharmacokinetics of paclitaxel-loaded lipid nanocapsules (LNC) in rats to assess the intrinsic effect of the dosage form on the improvement of paclitaxel oral exposure.MethodsPaclitaxel-loaded LNC were prepared and characterized in terms of size distribution, drug payload, and the kinetics of paclitaxel crystallization. Taxol®, Taxol® with verapamil, or paclitaxel-loaded LNC were administered orally to rats. The plasma concentration of paclitaxel was determined using liquid chromatography mass spectrometry.ResultsThe average size of LNC was 60.9 ± 1.5 nm. The drug payload of paclitaxel was 1.91 ± 0.01 mg/g of aqueous dispersion. The encapsulation efficiency was 99.9 ± 1.0%, and 1.7 ± 0.1% of paclitaxel was crystallized after 24 h. The oral bioavailability of Taxol® alone was 6.5%. After oral administration of paclitaxel-loaded LNC or paclitaxel associated with verapamil, the area under the plasma concentration–time curve was significantly increased (about 3-fold) in comparison to the control group (p < 0.05).ConclusionsThe results indicated that LNC provided a promising new formulation to enhance the oral bioavailability of paclitaxel while avoiding the use of pharmacologically active P-gp inhibitors, such as verapamil.