Sustained release of 5-FU from Poloxamer gels interpenetrated by crosslinking chitosan network

Int J Pharm. 2009 Dec 1;382(1-2):39-44. doi: 10.1016/j.ijpharm.2009.07.035. Epub 2009 Aug 8.

Abstract

This study investigates in vitro the drug delivery characteristics of new thermo-sensitive gels, P-CS/GA gels, in which a chitosan (CS) network is crosslinked with various concentrations of glutaraldehyde (GA) that interpenetrates Poloxamer (P) gels. The results indicate that the swelling ratios of all P-CS/GA gels are markedly superior to those of non-swelling P and P-CS gels. For example, P-CS/GA (0.1 wt.%) gels have swelling ratios of 13.2+/-1.0, which are maintained for approximately 18 h in water at 37 degrees C. In vitro releases of 5-FU from P-CS/GA (0.1 wt.%) gels had significantly lower initial burst release (P<0.01) and lasted much longer than those from gels without a CS network. For example, the duration of release of 5-FU was in a significantly sustained manner for up to 52 h, which was about 10 times or longer than the period of delivery using P or P-CS gels. The release of drugs from gels with an interpenetrating CS network could be modeled by Fickian diffusion; the characteristic constant 'k' of drug-gel systems decreased as increasing GA concentrations in the P-CS/GA gels, and increasing the viscosities of the P, P-CS and P-CS/GA solutions.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antimetabolites, Antineoplastic / chemistry*
  • Chemistry, Pharmaceutical
  • Chitosan / chemistry*
  • Cross-Linking Reagents / chemistry*
  • Delayed-Action Preparations
  • Diffusion
  • Drug Carriers*
  • Drug Compounding
  • Fluorouracil / chemistry*
  • Gels
  • Glutaral / chemistry*
  • Kinetics
  • Models, Chemical
  • Molecular Conformation
  • Poloxamer / chemistry*
  • Solubility
  • Temperature
  • Viscosity

Substances

  • Antimetabolites, Antineoplastic
  • Cross-Linking Reagents
  • Delayed-Action Preparations
  • Drug Carriers
  • Gels
  • Poloxamer
  • Chitosan
  • Glutaral
  • Fluorouracil