Taro-corms mucilage-alginate microspheres for the sustained release of pregabalin: In vitro &in vivo evaluation

Int J Biol Macromol. 2019 Oct 15:139:1191-1202. doi: 10.1016/j.ijbiomac.2019.08.100. Epub 2019 Aug 12.

Abstract

Taro corms mucilage (TCM)-alginate microspheres had been prepared using TCM and alginate as blend and coated form in various ratios through inotropic gelation approach. The prepared microspheres have been of sphere-formed having coarse surface with average particle size within the range 498 μm ± 0.17 to 715 μm ± 0.34. The drug entrapment efficiency was 74.33 ± 0.04% to 89.63 ± 0.01% and swelling of microspheres followed the pattern (blended >coated >plain). FTIR research showed that there had been no interactions among pregabalin and polymers used; these microspheres were further characterized by DSC and XRD. The in vitro drug release followed sustained release (Korsmeyer-Peppas model) pattern (R2 = 0.9552-0.9906) and value of n > 1 showed that drug released by means of anomalous (non-Fickian) diffusion. The in vivo research established that there were highly significant difference with p < 0.001 within the pharmacokinetic parameters (Cmax, t½, AUC0-∞, Ke), while pregabalin microspheres in comparison to pure drug. Therefore, it is concluded that blended microspheres has greater bioavailability for pregabalin with sustained release effect. This evolved that TCM has been proved to be emerging potential pharmaceutical excipient for sustained release drug delivery systems.

Keywords: Microspheres; Pharmacokinetic parameters; Pregabalin; Sustained; Taro corms mucilage.

MeSH terms

  • Alginates / chemistry*
  • Animals
  • Colocasia / chemistry*
  • Delayed-Action Preparations
  • Drug Carriers / chemistry*
  • Male
  • Microspheres*
  • Plant Mucilage / chemistry*
  • Pregabalin / chemistry*
  • Pregabalin / pharmacokinetics
  • Rabbits
  • Rheology
  • Tissue Distribution

Substances

  • Alginates
  • Delayed-Action Preparations
  • Drug Carriers
  • Plant Mucilage
  • Pregabalin