New MultiPEG-conjugated theophylline derivatives: synthesis and pharmacological evaluations

Eur J Pharm Sci. 2007 Mar;30(3-4):343-50. doi: 10.1016/j.ejps.2006.12.001. Epub 2006 Dec 14.

Abstract

The successful conjugation of active theophylline molecules to two new multifunctional high-molecular weight poly(ethylene glycol) derivatives (MultiPEG) and their pharmacokinetic evaluations are reported. The drug loading was increased up to six times in comparison with commercial PEG of the same molecular weight. A clear increase of the time of persistence within the body and a concomitant improvement of the overall pharmacokinetic properties of those prodrugs were also observed. These studies sustain the use of these new PEG-based polymeric supports as a valuable alternative for an effective drug delivery system.

MeSH terms

  • Animals
  • Area Under Curve
  • Biotransformation
  • Bronchodilator Agents / chemistry
  • Bronchodilator Agents / pharmacokinetics*
  • Bronchodilator Agents / toxicity
  • Chemical Phenomena
  • Chemistry, Physical
  • Chromatography, High Pressure Liquid
  • Drug Delivery Systems
  • Female
  • Magnetic Resonance Spectroscopy
  • Male
  • Mice
  • Mice, Inbred ICR
  • Molecular Weight
  • Polyethylene Glycols / chemistry*
  • Polyethylene Glycols / pharmacokinetics*
  • Rabbits
  • Rats
  • Spectrophotometry, Ultraviolet
  • Theophylline / analogs & derivatives*
  • Theophylline / chemistry
  • Theophylline / pharmacokinetics*

Substances

  • Bronchodilator Agents
  • Polyethylene Glycols
  • Theophylline