Pharmaceutical Research

, Volume 23, Issue 6, pp 1243–1250 | Cite as

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

  • Sandra Peltier
  • Jean-Michel Oger
  • Frédéric Lagarce
  • William Couet
  • Jean-Pierre BenoîtEmail author
Research Paper


The 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.


Paclitaxel-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.


The 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).


The 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.

Key Words

nanocapsule oral bioavailability paclitaxel pharmacokinetics P-glycoprotein inhibitor 



lipid nanocapsules





We are very grateful to Pierre Legras and Jerome Roux from the animal house of the Medical College of Angers for skilful technical support. We would also like to thank Drs. Claire Dulieu and Didier Bazile from Mainelab/Ethypharm for supplying the batches of lipid nanocapsules. This work was supported by grants from the “Fondation pour la Recherche Médicale”, the “Comité départemental du Maine-et-Loire de la Ligue contre le Cancer”, and the “Association pour la Recherche sur le Cancer”.


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Copyright information

© Springer Science + Business Media, Inc. 2006

Authors and Affiliations

  • Sandra Peltier
    • 1
  • Jean-Michel Oger
    • 1
  • Frédéric Lagarce
    • 1
  • William Couet
    • 2
  • Jean-Pierre Benoît
    • 1
    Email author
  1. 1.U646, Angers, F-49100 FranceUniversité d'AngersAngersCedex1France
  2. 2.EA3809, Pharmacologie des Agents Anti-InfectieuxFaculté de Médecine & PharmaciePoitiersFrance

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