Synthesis of fenoprofen and gemfibrozil styrene-maleic acid copolymer conjugates

Acta Pharm. 2005 Jun;55(2):169-76.

Abstract

Two types of polymer-drug conjugates were synthesized starting from styrene-maleic acid anhydride copolymer (SMA). Fenoprofen and gemfibrozil were chosen as model drugs because of their short plasma half lives. Both drugs were first converted to their 2-aminoethylamides, which possess free amino groups capable of reacting with SMA anhydride rings. By modifying the degree and type of substitution, lipophilic and hydrophilic conjugates were obtained. Drug loading in the conjugates was between 17 and 47%.

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis*
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Chromatography, Thin Layer
  • Fenoprofen / analogs & derivatives*
  • Fenoprofen / chemical synthesis*
  • Fenoprofen / chemistry
  • Gemfibrozil / analogs & derivatives*
  • Gemfibrozil / chemical synthesis*
  • Gemfibrozil / chemistry
  • Hypolipidemic Agents / chemical synthesis*
  • Hypolipidemic Agents / chemistry
  • Maleates / chemistry
  • Prodrugs
  • Spectrophotometry, Infrared
  • Spectrophotometry, Ultraviolet
  • Spectroscopy, Fourier Transform Infrared
  • Styrenes / chemistry

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Hypolipidemic Agents
  • Maleates
  • Prodrugs
  • Styrenes
  • maleic acid
  • Gemfibrozil
  • Fenoprofen