Effects of amphiphilic PCL-PEG-PCL copolymer addition on 5-fluorouracil release from biodegradable PCL films for stent application

Int J Pharm. 2011 Oct 31;419(1-2):77-84. doi: 10.1016/j.ijpharm.2011.07.020. Epub 2011 Jul 23.

Abstract

Biodegradable film-based stents emerged as a promising medical platform for drug delivery to resolve stenosis encountered in physiological conduits (e.g. blood vessels, biliary and urethral tracts). Drug release kinetics significantly affects the pharmacological effects of a stent, thus it is desirable for a stent to possess highly adjustable drug release kinetics. In this study, a series of amphiphilic poly(ɛ-caprolactone)-poly(ethylene glycol)-poly(ɛ-caprolactone) (PCL-PEG-PCL) copolymers were used as additives to adjust 5-fluorouracil (5-FU) release from PCL films. The effects of the copolymer addition on drug release behavior, drug permeability, crystalline states, and surface and internal morphologies of the films were investigated. It was found that, the addition of PCL-PEG-PCL could accelerate 5-FU release. The release rate of 5-FU increased with increasing content of PCL-PEG-PCL in the film, but it decreased with the ratio of PCL blocks in the PCL-PEG-PCL copolymer. The diffusion test results showed that 5-FU diffused through the film containing PCL-PEG-PCL faster than it permeated through the pure PCL film, indicating that the addition of PCL-PEG-PCL can improve the permeability of 5-FU in PCL film. The addition of PCL-PEG-PCL copolymer showed high drug-release-regulating ability in the 5-FU-loaded PCL films.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antimetabolites, Antineoplastic / administration & dosage*
  • Crystallization
  • Drug Carriers / chemistry
  • Drug-Eluting Stents*
  • Fluorouracil / administration & dosage*
  • Permeability
  • Polyesters / chemistry*
  • Polyethylene Glycols / chemistry*

Substances

  • Antimetabolites, Antineoplastic
  • Drug Carriers
  • Polyesters
  • poly(epsilon-caprolactone)-b-poly(ethyleneglycol)-b-poly(epsilon-caprolactone)
  • Polyethylene Glycols
  • Fluorouracil