Pharmacokinetics and organ distribution of fluorescein in experimental pigs: an input study for confocal laser endomicroscopy of the gastrointestinal tract

Neuro Endocrinol Lett. 2010:31 Suppl 2:57-61.

Abstract

Objective: Confocal laser scanning endomicroscopy (CLSE) is a diagnostic technology that produces virtual histology of the mucosal layer using fluorescence technique. Fluorescein (FSC) is the most commonly used fluorescence agent. Fluorescence light coming from a horizontal special focal plane is detected during confocal laser endomicroscopy of the gastrointestinal tract. FSC causes intensive yellowish discoloration of tissues, including skin and mucous membranes. This pre-clinical study was aimed to evaluate the tissue distribution and pharmacokinetics of FSC after its intravenous administration.

Methods: The study was performed in an adult experimental pig. A reversed-phase high-performance liquid chromatographic method with fluorescence detection was used for the determination of fluorescein in blood plasma and tissue samples.

Results and conclusion: The pharmacokinetic study of fluorescein determined the optimum time interval for diagnostic scanning (5-10 min.) The biodistribution study of fluorescein (aimed on the potential organ accumulation) proved the high concentration in the renal system followed by levels in bile > lung > adipose tissue > all other organs (including gastrointestinal wall) and these were relatively similar to each other. Fluorescein has a significantly low distribution in the brain (contrast with the level in adipose tissue indicates the low ability to penetrate the blood-brain barrier).

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adipose Tissue / cytology
  • Adipose Tissue / metabolism
  • Animals
  • Blood-Brain Barrier
  • Brain / cytology
  • Brain / metabolism
  • Female
  • Fluorescein / administration & dosage
  • Fluorescein / pharmacokinetics*
  • Fluorescent Dyes / administration & dosage
  • Fluorescent Dyes / pharmacokinetics*
  • Gastrointestinal Tract / cytology
  • Gastrointestinal Tract / metabolism*
  • Injections, Intravenous
  • Kidney / cytology
  • Kidney / metabolism
  • Lung / cytology
  • Lung / metabolism
  • Microscopy, Confocal*
  • Models, Animal
  • Swine

Substances

  • Fluorescent Dyes
  • Fluorescein