Preparation and Characterization of a Lutein Solid Dispersion to Improve Its Solubility and Stability
- Authors
- Lim, C.; Kang, J.K.; Jung, C.E.; Sim, T.; Her, J.; Kang, K.; Lee, E.S.; Youn, Y.S.; Choi, H.-G.; Oh, K.T.
- Issue Date
- 2-Jun-2021
- Publisher
- Springer Science and Business Media Deutschland GmbH
- Keywords
- absorption; bioavailability; degradation; lutein; oral drug delivery; pH sensitivity; solid dispersion; stability
- Citation
- AAPS PharmSciTech, v.22, no.5
- Journal Title
- AAPS PharmSciTech
- Volume
- 22
- Number
- 5
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/62364
- DOI
- 10.1208/s12249-021-02036-4
- ISSN
- 1530-9932
1522-1059
- 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. Graphical abstract: [Figure not available: see fulltext.]. © 2021, American Association of Pharmaceutical Scientists.
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