Examination of dissolution ratio of β-carotene in water for practical application of β-carotene amorphous solid dispersion

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Abstract
β-Carotene (BC) has an antioxidant effect that removes active oxygen in vivo and can reduce the risk of developing various diseases, but it is almost insoluble in water. Therefore, to develop highly effective BC functional food products, it is essential to increase its water solubility, which in turn can improve its absolute bioavailability. Recently, a BC amorphous solid dispersion (BC-SD) prepared using hot melt extruder technology had increased water solubility and improved absorption from the gastrointestinal tract. However, only a part of the BC in BC-SD could be dissolved in water. In this study, we evaluated whether the dissolution ratio of BC in water could be improved by examining the mixing ratio of BC and base materials in BC-SD. Results showed that by reducing the mixing ratio of BC to the base materials, the dissolution ratio of BC in water increased. It was also found that when BC-SD, which has the highest dissolution ratio, was intragastrically administered to rats, its absolute bioavailability was most increased. These results are useful findings that may help in reducing the costs associated with the BC-SD manufacturing process and will be an important part of our strategy for practical use in the future.
Funding Information
  • Platform Project for Supporting Drug Discovery and Life Science Research (Basis for Supporting Innovative Drug Discovery and Life Science Research (BINDS)) from AMED (JP20am0101084 and JP20am0101123)

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