Study on hydrophilic 5-fluorouracil release from hydrophobic poly(ε-caprolactone) cylindrical implants

Drug Dev Ind Pharm. 2011 Sep;37(9):1068-75. doi: 10.3109/03639045.2011.559658. Epub 2011 Mar 30.

Abstract

Hydrophilic 5-fluorouracil (5-FU) loaded cylindrical poly(ε-caprolactone) (PCL) implants with different implant diameters (2, 4 and 8 mm), different drug loadings (25% and 50%) and end-capping were fabricated and characterized. The implant structure, drug content and molecular weight of PCL after 120 days drug release were investigated. The in vitro release results showed that, when the drug loading was the same, drug release was fastest for the implant with a diameter of 2 mm and slowest for the implant with a diameter of 8 mm; for the implants with the same diameters, the release of drug from the implants with 50% drug loading was faster than that from the implants with 25% drug loading; however, this effect of drug loading decreased with the increase of implant diameter; in addition, 5-FU was released slightly slower from the end-capped implants than from the corresponding uncapped implants; the drug release data for all the uncapped implants were best fit with the Ritger-Peppas model. Drug release from the hydrophobic implants was found to be dominated by diffusion mechanism. Scanning electron microscopy images and drug content measurements revealed that 5-FU release took place gradually from the exterior region to the interior region of the implants.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biological Availability
  • Drug Carriers / chemistry*
  • Drug Implants*
  • Fluorouracil / pharmacokinetics*
  • Hydrophobic and Hydrophilic Interactions
  • Models, Chemical
  • Polyesters / chemistry*

Substances

  • Drug Carriers
  • Drug Implants
  • Polyesters
  • polycaprolactone
  • Fluorouracil