Release Kinetics of 5-fluorouracil-loaded Microspheres on an Experimental Rat Glioma

Anticancer Res. Jan-Feb 2003;23(1A):21-5.

Abstract

Background: Biodegradable loaded systems are promising devices for controlled and sustained release of anticancer drugs to brain tumours. We investigated the influence of drug-release profiles of 5-fluorouracil-loaded microspheres designed for the treatment of malignant gliomas.

Materials and methods: 2.5 mg 5-FU delivered by either fast. (1 formulation) or slow-(2 formulations) 5-FU release microspheres (MS) were tested in C6-glioma rat brains. Tumor response was assessed by T2-weighted MRI.

Results: All treated animals, whatever the release profile considered, displayed a comparable 50% increase in life span versus controls. Delays in C6-glioma development appeared to correspond to the in vitro release periods of MS. In terms of curative prospect, complete remission was only observed in 11% of 5-FU-treated animals (4 out of 38).

Conclusion: Formulation was unambiguously implicated in the response observed after local delivery of 5-FU to glioma.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antimetabolites, Antineoplastic / administration & dosage
  • Antimetabolites, Antineoplastic / chemistry
  • Antimetabolites, Antineoplastic / pharmacokinetics*
  • Brain Neoplasms / drug therapy
  • Brain Neoplasms / metabolism*
  • Chemistry, Pharmaceutical
  • Delayed-Action Preparations
  • Female
  • Fluorouracil / administration & dosage
  • Fluorouracil / chemistry
  • Fluorouracil / pharmacokinetics*
  • Glioma / drug therapy
  • Glioma / metabolism*
  • Magnetic Resonance Imaging
  • Microspheres
  • Rats
  • Rats, Sprague-Dawley

Substances

  • Antimetabolites, Antineoplastic
  • Delayed-Action Preparations
  • Fluorouracil