Development of pH-sensitive pectinate/alginate microspheres for colon drug delivery

J Mater Sci Mater Med. 2013 Feb;24(2):317-23. doi: 10.1007/s10856-012-4798-9. Epub 2012 Oct 27.

Abstract

The purposes of this study were to develop and evaluate calcium pectinate/alginate microspheres (PAMs) and to exploit their pH-sensitive properties for colon-targeted delivery of encapsulated cisplatin. PAMs were prepared using an electrospraying method. The PAMs, as cores, were then coated with Eudragit S100 using a polyelectrolyte multilayer coating technique in aqueous solution. The morphology of the microspheres was observed under scanning electron microscopy. In vitro drug release studies were performed in simulated gastrointestinal fluid, and the results indicated that approximately 5 % of the cisplatin was released from the Eudragit S100-coated PAMs, and 51 % of the cisplatin was released from the uncoated PAMs at 1 h. The release of cisplatin from the Eudragit S100-coated PAMs was more sustained in simulated gastric fluid than in simulated intestinal fluid due to the increased solubility of the coating polymer in media with pH >7.0. Drug release from the Eudragit S100-coated PAMs was best described by the Higuchi's square root model. From these results, it was concluded that Eudragit S100-coated PAMs are a potential carrier for delivery of cisplatin to the colon.

MeSH terms

  • Alginates / chemical synthesis
  • Alginates / chemistry*
  • Cisplatin / administration & dosage*
  • Cisplatin / pharmacokinetics
  • Coated Materials, Biocompatible / chemical synthesis
  • Coated Materials, Biocompatible / chemistry
  • Colon* / metabolism
  • Drug Carriers / analysis
  • Drug Carriers / chemical synthesis
  • Drug Carriers / chemistry
  • Drug Delivery Systems* / methods
  • Excipients / analysis
  • Excipients / chemistry
  • Gastrointestinal Contents
  • Glucuronic Acid / chemical synthesis
  • Glucuronic Acid / chemistry
  • Hexuronic Acids / chemical synthesis
  • Hexuronic Acids / chemistry
  • Humans
  • Hydrogen-Ion Concentration
  • Materials Testing
  • Microspheres*
  • Particle Size
  • Pectins / chemical synthesis
  • Pectins / chemistry*
  • Polymethacrylic Acids / chemistry
  • Solubility

Substances

  • Alginates
  • Coated Materials, Biocompatible
  • Drug Carriers
  • Excipients
  • Hexuronic Acids
  • Polymethacrylic Acids
  • methylmethacrylate-methacrylic acid copolymer
  • Pectins
  • Glucuronic Acid
  • Cisplatin