Tranexamic acid loaded gellan gum-based polymeric microbeads for controlled release: in vitro and in vivo assessment

Colloids Surf B Biointerfaces. 2013 Dec 1:112:483-91. doi: 10.1016/j.colsurfb.2013.07.054. Epub 2013 Aug 8.

Abstract

Gellan gum (GG) microbeads containing tranexamic acid (TA), an anti-fibrinolytic drug were prepared by a classic sol-gel transition induced by ionic crosslinking technique using aluminum chloride (AlCl3) as cross-linking agent. The influence of different formulation variables on in vitro physico-chemical parameters and drug release studies were performed systematically. The microbeads were evaluated by scanning electron microscopy (SEM), Fourier transform infra-red (FTIR) spectroscopy, X-ray diffraction (XRD), differential scanning calorimetry (DSC) and high performance liquid chromatographic (HPLC) analysis. Particle size and swelling behavior of microbeads were also investigated. Microbeads showed improved drug encapsulation efficiency along with enhanced drug release. The in vivo studies exhibited sustained drug release in rabbits over a prolonged period after oral administration of these newly developed TA loaded GG microbeads. Based on the results of in vitro and in vivo studies in experimental animal model it was concluded that these microbeads provided intestinal specific controlled release of TA.

Keywords: Controlled release; Gellan gum; Microbeads; Sol–gel transition; Tranexamic acid.

MeSH terms

  • Animals
  • Antifibrinolytic Agents / administration & dosage
  • Antifibrinolytic Agents / blood
  • Antifibrinolytic Agents / pharmacokinetics
  • Cross-Linking Reagents
  • Delayed-Action Preparations / chemistry*
  • Drug Carriers / chemistry*
  • Drug Compounding / methods
  • Drug Delivery Systems*
  • Female
  • Hydrogels
  • Male
  • Microscopy, Electron, Scanning
  • Microspheres
  • Particle Size
  • Polysaccharides, Bacterial / chemistry*
  • Rabbits
  • Spectroscopy, Fourier Transform Infrared
  • Thermodynamics
  • Tranexamic Acid / administration & dosage*
  • Tranexamic Acid / blood
  • Tranexamic Acid / pharmacokinetics
  • X-Ray Diffraction

Substances

  • Antifibrinolytic Agents
  • Cross-Linking Reagents
  • Delayed-Action Preparations
  • Drug Carriers
  • Hydrogels
  • Polysaccharides, Bacterial
  • Tranexamic Acid
  • gellan gum