Hyaluronic acid based micelle for articular delivery of triamcinolone, preparation, in vitro and in vivo evaluation

Int J Pharm. 2015 Jul 15;489(1-2):218-25. doi: 10.1016/j.ijpharm.2015.05.001. Epub 2015 May 5.

Abstract

A novel triamcinolone loaded polymeric micelle was synthesized based on hyaluronic acid and phospholipid for articular delivery. The newly developed micelle was characterized for physicochemical properties including size, zeta potential, differential scanning calorimetry (DSC) analysis and also morphology by means of transmission electron microscopy. The biocompatibility of micelle was explored by histopathological experiment in rat model. Also biological fate of micelle was investigated in rat by means of real time in vivo imaging system. Triamcinolone loaded micelle was in the size range of 186 nm with negative zeta potential charge. Micelles were spherical in shape with core shell like structure. Triamcinolone was released from micelle during 76 h with almost low burst effect. DSC analysis showed the conversion of crystalline triamcinolone from its crystalline state. Histopathological analysis showed no evidence of tissue damage or phagocytic accumulation in knee joint of rat. The real time in vivo imaging analysis suggested at least three days retention time of micellar system in knee joint post injection.

Keywords: Articular delivery; Hyaluronic acid; In vivo real time imaging; Polymeric micelle; Triamcinolone.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents* / administration & dosage
  • Anti-Inflammatory Agents* / blood
  • Anti-Inflammatory Agents* / chemistry
  • Anti-Inflammatory Agents* / pharmacokinetics
  • Calorimetry, Differential Scanning
  • Drug Carriers* / administration & dosage
  • Drug Carriers* / chemistry
  • Drug Carriers* / pharmacokinetics
  • Drug Compounding
  • Drug Liberation
  • Hyaluronic Acid / chemistry*
  • Injections, Intra-Articular
  • Knee Joint / anatomy & histology
  • Knee Joint / drug effects
  • Male
  • Micelles
  • Microscopy, Electron, Transmission
  • Phosphatidylethanolamines / chemistry
  • Rats, Wistar
  • Triamcinolone* / administration & dosage
  • Triamcinolone* / blood
  • Triamcinolone* / chemistry
  • Triamcinolone* / pharmacokinetics

Substances

  • Anti-Inflammatory Agents
  • Drug Carriers
  • Micelles
  • Phosphatidylethanolamines
  • 1,2-distearoylphosphatidylethanolamine
  • Triamcinolone
  • Hyaluronic Acid