1. Preparation and Characterization of a Lutein Solid Dispersion to Improve Its Solubility and Stability
- Author
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Yu Seok Youn, Han-Gon Choi, Kioh Kang, Chan Eun Jung, Eun Seong Lee, Kyung Taek Oh, Jin Kook Kang, Chaemin Lim, Jaewon Her, and Taehoon Sim
- Subjects
Drug ,endocrine system ,Lutein ,Polymers ,media_common.quotation_subject ,Pharmaceutical Science ,Biological Availability ,02 engineering and technology ,Absorption (skin) ,Aquatic Science ,Methylcellulose ,030226 pharmacology & pharmacy ,Matrix (chemical analysis) ,03 medical and health sciences ,chemistry.chemical_compound ,Crystallinity ,0302 clinical medicine ,Drug Stability ,X-Ray Diffraction ,Drug Discovery ,Humans ,Solubility ,Dissolution ,Ecology, Evolution, Behavior and Systematics ,Chromatography, High Pressure Liquid ,media_common ,Chromatography ,Ecology ,Chemistry ,food and beverages ,General Medicine ,021001 nanoscience & nanotechnology ,eye diseases ,Bioavailability ,Drug Liberation ,Solvents ,sense organs ,0210 nano-technology ,Agronomy and Crop Science - 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.
- Published
- 2020