Skip to main content
padlock icon - secure page this page is secure

Enhanced Oral Bioavailability and Absorption Mechanism Study of N3-O-Toluyl-Fluorouracil-Loaded Liposomes

Buy Article:

$106.67 + tax (Refund Policy)

The present investigation attempts to increase oral absorption of N3-O-Toluyl-Fluorouracil (TFu), one of the new and effective 5-fluorouracil prodrugs, by employing liposomal techniques. TFu-loaded liposomes with different sizes all resulted in higher bioavailabilities than TFu aqueous suspensions after oral administration, and the gastrointestinal absorption increased with the reduction of liposome sizes. In order to investigate the enhancing absorption mechanism of TFu-loaded liposomes, the everted gut sac experiments were applied to examine the influences of different factors. It was found that the uptake increased linearly with the concentration of TFu while the intestinal permeability coefficients changed slightly and the absorption process fitted with the Fick's diffusion law in the range of 5∼20 g ยท mL−1. The oral absorption of TFu-loaded liposomes might be a non-carrier-mediated and energy-independent, passive transport way. The liposomal bilayer was not stable enough and proned to be degraded partly in gastrointestinal tract (drug entrapment efficiency reduced by 5%∼17%). The comparative studies between TFu-loaded liposomes and TFu solid lipid dispersions indicated that the two formulations had the same effects on enhancing the oral absorption of TFu. It could be concluded that it was the free drug but not the intact liposomes that penetrated the intestinal wall; the increased affinity between TFu-loaded liposomes and the gut liquid caused better dispersion of TFu in the gastrointestinal tract, prolonged the drug residence time in the absorption sites and resulted in better absorption effects. The decreasing liposomes sizes resulted in an increase in surface area, saturation solubility and consequently, and an increase in the bio-adhesion to the gastrointestinal tract wall thus increasing the oral bioavailability.
No Reference information available - sign in for access.
No Citation information available - sign in for access.
No Supplementary Data.
No Article Media
No Metrics


Document Type: Research Article

Publication date: March 1, 2008

More about this publication?
  • Journal of Biomedical Nanotechnology (JBN) is a peer-reviewed multidisciplinary journal providing broad coverage in all research areas focused on the applications of nanotechnology in medicine, drug delivery systems, infectious disease, biomedical sciences, biotechnology, and all other related fields of life sciences.
  • Editorial Board
  • Information for Authors
  • Subscribe to this Title
  • Terms & Conditions
  • Ingenta Connect is not responsible for the content or availability of external websites
  • Access Key
  • Free content
  • Partial Free content
  • New content
  • Open access content
  • Partial Open access content
  • Subscribed content
  • Partial Subscribed content
  • Free trial content
Cookie Policy
Cookie Policy
Ingenta Connect website makes use of cookies so as to keep track of data that you have filled in. I am Happy with this Find out more