Scintigraphic evaluation of the pharmacokinetics of a soluble polymeric drug carrier

Eur J Nucl Med. 1992;19(6):449-52. doi: 10.1007/BF00177374.

Abstract

There is a growing interest in the use of macro-molecular carriers for therapeutic agents. If these carriers can be labelled with an appropriate gamma-emitter, their biodistribution could be followed by scintigraphy. We have imaged the biodistribution of a synthetic branched polypeptide, based on a poly-L-lysine backbone (average molecular mass 45 kDa). The polymer was conjugated to diethylene triamine penta-acetic acid and labelled by chelation with indium-111. Mice were injected i.v. with labelled material and imaged with a gamma-camera with a pin-hole collimator. Images showed the majority of tracer remaining in the blood pool, but about 35% appeared in the urinary bladder within 1.5 h. When the 111In-polymer was fractionated by gel filtration chromatography on S-300, the imaging showed that the early eluting material was retained, the intermediate showed some renal clearance, and the late was rapidly excreted. These findings show the value of gamma-scintigraphy for biodistribution studies with such polymeric drug carriers and its potential for clinical pharmacokinetic studies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Drug Carriers*
  • Indium Radioisotopes*
  • Mice
  • Mice, Inbred BALB C
  • Pentetic Acid
  • Polymers
  • Tissue Distribution

Substances

  • Drug Carriers
  • Indium Radioisotopes
  • Polymers
  • Pentetic Acid