Alginate gel-coated oil-entrapped alginate-tamarind gum-magnesium stearate buoyant beads of risperidone

Int J Biol Macromol. 2015:78:102-11. doi: 10.1016/j.ijbiomac.2015.04.001. Epub 2015 Apr 8.

Abstract

A novel alginate gel-coated oil-entrapped calcium-alginate-tamarind gum (TG)-magnesium stearate (MS) composite floating beads was developed for intragastric risperidone delivery with a view to improving its oral bioavailability. The TG-blended alginate core beads containing olive oil and MS as low-density materials were accomplished by ionotropic gelation technique. Effects of polymer-blend ratio (sodium alginate:TG) and crosslinker (CaCl2) concentration on drug entrapment efficiency (DEE, %) and cumulative drug release after 8 h (Q8h, %) were studied to optimize the core beads by a 3(2) factorial design. The optimized beads (F-O) exhibited DEE of 75.19±0.75% and Q8h of 78.04±0.38% with minimum errors in prediction. The alginate gel-coated optimized beads displayed superior buoyancy and sustained drug release property. The drug release profiles of the drug-loaded uncoated and coated beads were best fitted in Higuchi kinetic model with Fickian and anomalous diffusion driven mechanisms, respectively. The optimized beads yielded a notable sustained drug release profile as compared to marketed immediate release preparation. The uncoated and coated Ca-alginate-TG-MS beads were also characterized by SEM, FTIR and P-XRD analyses. Thus, the newly developed alginate-gel coated oil-entrapped alginate-TG-MS composite beads are suitable for intragastric delivery of risperidone over a prolonged period of time.

Keywords: Alginate; Emulsion gel beads; Tamarind gum.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alginates / chemistry*
  • Chemistry, Pharmaceutical
  • Drug Liberation
  • Gels / chemistry*
  • Glucuronic Acid / chemistry
  • Hexuronic Acids / chemistry
  • Magnesium / chemistry*
  • Microspheres*
  • Particle Size
  • Plant Gums / chemistry*
  • Risperidone / administration & dosage*
  • Spectroscopy, Fourier Transform Infrared
  • Stearic Acids / chemistry*
  • Tamarindus / chemistry*
  • X-Ray Diffraction

Substances

  • Alginates
  • Gels
  • Hexuronic Acids
  • Plant Gums
  • Stearic Acids
  • stearic acid
  • Glucuronic Acid
  • Magnesium
  • Risperidone