Synthesis and characterization of biocompatible poly(organophosphazenes) aiming for local delivery of protein drugs

Int J Pharm. 2006 May 11;314(1):90-6. doi: 10.1016/j.ijpharm.2006.02.009. Epub 2006 Feb 23.

Abstract

Biocompatible and thermosensitive poly(organophosphazenes) with a lower critical solution temperature (LCST) below body temperature have been designed with the aim for the local delivery of peptide and protein drugs. These polymers could be synthesized by introducing short chain tri- or tetraethylene glycol as a hydrophilic group and a dipeptide, GlyGluEt2 as a hydrophobic group into the polyphosphazene backbone. The local tolerance tests using rabbits have shown that our polymers are biocompatible. Using the amphiphilic properties of these polymers, in vitro studies were performed for loading and releasing of a human growth hormone (hGH) as a model drug. The entrapment efficiency (%) of hGH by the polymer decreased as its polymer concentration increased, but exhibited high efficiency of more than 95% even at 20% hGH concentration in the polymer. The entrapped hGH has shown to be controlled releasing for 3-4 days.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Biocompatible Materials / chemistry
  • Dipeptides / chemistry
  • Drug Delivery Systems
  • Drug Stability
  • Ethylene Glycols / chemistry
  • Hot Temperature
  • Human Growth Hormone / administration & dosage
  • Human Growth Hormone / chemistry
  • Male
  • Peptides / administration & dosage
  • Peptides / chemistry*
  • Phosphoranes / chemical synthesis*
  • Phosphoranes / chemistry
  • Polymers / chemistry*
  • Proteins / administration & dosage
  • Proteins / chemistry*
  • Rabbits
  • Recombinant Proteins / administration & dosage
  • Recombinant Proteins / chemistry
  • Solubility

Substances

  • Biocompatible Materials
  • Dipeptides
  • Ethylene Glycols
  • Peptides
  • Phosphoranes
  • Polymers
  • Proteins
  • Recombinant Proteins
  • Human Growth Hormone
  • hexachlorocyclotriphosphazene