Preparation and Characterization of a Lutein Solid Dispersion to Improve Its Solubility and Stability

AAPS PharmSciTech. 2021 Jun 2;22(5):169. doi: 10.1208/s12249-021-02036-4.

Abstract

Lutein has been used as a dietary supplement for the treatment of eye diseases, especially age-related macular degeneration. For oral formulations, we investigated lutein stability in artificial set-ups mimicking different physiological conditions and found that lutein was degraded over time under acidic conditions. To enhance the stability of lutein upon oral intake, we developed enteric-coated lutein solid dispersions (SD) by applying a polymer, hydroxypropyl methylcellulose acetate succinate (HPMCAS-LF), through a solvent-controlled precipitation method. The SD were characterized in crystallinity, morphology, and drug entrapment. In the dissolution profile of lutein SD, a F80 formulation showed resistance toward the acidic environment under simulated gastric conditions while exhibiting a bursting drug release under simulated intestinal conditions. Our results highlight the potential use of HPMCAS-LF as an effective matrix to enhance lutein bioavailability during oral delivery and to provide novel insights into the eye-care supplement industry, with direct benefits for the health of patients.

Keywords: absorption; bioavailability; degradation; lutein; oral drug delivery; pH sensitivity; solid dispersion; stability.

MeSH terms

  • Biological Availability
  • Chromatography, High Pressure Liquid / methods
  • Drug Liberation
  • Drug Stability
  • Humans
  • Lutein / chemical synthesis*
  • Lutein / pharmacokinetics*
  • Methylcellulose / analogs & derivatives*
  • Methylcellulose / chemical synthesis
  • Methylcellulose / pharmacokinetics
  • Polymers / chemical synthesis
  • Polymers / pharmacokinetics
  • Solubility
  • Solvents
  • X-Ray Diffraction / methods

Substances

  • Polymers
  • Solvents
  • hydroxypropylmethylcellulose acetate succinate
  • Methylcellulose
  • Lutein