Metal ion-induced alginate-locust bean gum IPN microspheres for sustained oral delivery of aceclofenac

Int J Biol Macromol. 2015 Jan:72:47-53. doi: 10.1016/j.ijbiomac.2014.07.054. Epub 2014 Aug 9.

Abstract

The alginate microspheres represent a useful tool for sustained oral delivery of drugs but exhibit several problems associated with the stability and rapid release of drugs at higher pH values. To overcome these drawbacks, alginate-locust bean gum (LBG) interpenetrating microspheres were prepared by calcium ion (Ca(+2)) induced ionotropic gelation technique for prolonged release of aceclofenac. The drug entrapment efficiency of these microspheres was found to be 59-93%. The microspheres lied in the size range of 406-684μm. Scanning electron microscopy revealed spherical shape of the microspheres. No drug-polymer interaction was evident after infrared spectroscopy analysis. The microspheres provided sustained release of aceclofenac in phosphate buffer solution (pH 6.8) over a period of 8h. The drug release data were fitted into the Korsmeyer-Peppas model and the drug release was found to follow anomalous (non-Fickian) diffusion mechanism. Pharmacodynamic study of the microspheres showed a prolonged anti-inflammatory activity in carrageenan-induced rat paw model following oral administration.

Keywords: Alginate; Anti-inflammatory activity; Locust bean gum; Microspheres; Sustained drug delivery.

MeSH terms

  • Administration, Oral
  • Alginates / chemistry*
  • Animals
  • Anti-Inflammatory Agents / pharmacology
  • Diclofenac / administration & dosage
  • Diclofenac / analogs & derivatives*
  • Diclofenac / pharmacology
  • Diclofenac / therapeutic use
  • Drug Delivery Systems*
  • Edema / drug therapy
  • Edema / pathology
  • Galactans / chemistry*
  • Glucuronic Acid / chemistry
  • Hexuronic Acids / chemistry
  • Ions
  • Mannans / chemistry*
  • Metals / chemistry*
  • Microscopy, Electron, Scanning
  • Microspheres*
  • Particle Size
  • Plant Gums / chemistry*
  • Polymers / chemistry*
  • Rats, Sprague-Dawley
  • Spectroscopy, Fourier Transform Infrared

Substances

  • Alginates
  • Anti-Inflammatory Agents
  • Galactans
  • Hexuronic Acids
  • Ions
  • Mannans
  • Metals
  • Plant Gums
  • Polymers
  • Diclofenac
  • Glucuronic Acid
  • aceclofenac
  • locust bean gum