Ciclosporin-loaded poly(lactide) microparticles: effect of TPGS

J Microencapsul. 2009 Feb;26(1):9-17. doi: 10.1080/02652040802094402.

Abstract

The properties of spray dried PLA microparticles were affected by the choice of solvents, amount of ciclosporin and TPGS added. Ethyl acetate formed microparticle with smooth surface when compared to those produced by dichloromethane. The results of FTIR have not shown chemical interaction amongst PLA, ciclosporin and TPGS while thermal analysis showed physical interactions amongst these components. TPGS was found to lower Tg value of PLA by exerting a plasticizing effect while ciclosporin reverted this effect. When the content of TPGS increased from 2% (w/w) to 10% (w/w), the microparticles tended to agglomerate due to the lowering of the polymer Tg values at the employed spray drying temperature. In addition, a lesser amount of ciclosporin was found at the surface of the microparticle and resulted in smaller initial release of ciclosporin. When 2% (w/w) TPGS was used, the initial release of ciclosporin was enhanced and the microparticles formed were not agglomerated.

MeSH terms

  • Cyclosporine / administration & dosage*
  • Cyclosporine / pharmacokinetics
  • Drug Carriers / chemistry
  • Lactic Acid*
  • Microspheres*
  • Plasticizers / chemistry
  • Polyesters
  • Polyethylene Glycols
  • Polymers*
  • Solvents
  • Vitamin E / analogs & derivatives*

Substances

  • Drug Carriers
  • Plasticizers
  • Polyesters
  • Polymers
  • Solvents
  • Vitamin E
  • Lactic Acid
  • Polyethylene Glycols
  • poly(lactide)
  • Cyclosporine
  • tocophersolan