Enhanced Oral Paclitaxel Bioavailability After Administration of Paclitaxel-Loaded Lipid Nanocapsules
作者： Sandra Peltier , Jean-Michel Oger , Frédéric Lagarce , William Couet , Jean-Pierre Benoît
DOI: 10.1007/S11095-006-0022-2
关键词: Dosage form 、 Oral administration 、 Intestinal absorption 、 Paclitaxel 、 Distribution (pharmacology) 、 Bioavailability 、 Chemistry 、 Pharmacokinetics 、 Chromatography 、 Pharmacology 、 Verapamil
摘要: The aim of this study was to evaluate the pharmacokinetics paclitaxel-loaded lipid nanocapsules (LNC) in rats assess intrinsic effect dosage form on improvement paclitaxel oral exposure. Paclitaxel-loaded LNC were prepared and characterized terms size distribution, drug payload, kinetics crystallization. Taxol®, Taxol® with verapamil, or administered orally rats. plasma concentration determined using liquid chromatography mass spectrometry. average 60.9 ± 1.5 nm. payload 1.91 0.01 mg/g aqueous dispersion. encapsulation efficiency 99.9 1.0%, 1.7 0.1% crystallized after 24 h. bioavailability alone 6.5%. After administration associated area under concentration–time curve significantly increased (about 3-fold) comparison control group (p < 0.05). results indicated that provided a promising new formulation enhance while avoiding use pharmacologically active P-gp inhibitors, such as verapamil.
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