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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.

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Data availability

The datasets during and/or analysed during the current study available from the corresponding author on reasonable request.

Abbreviations

BC:

β-Carotene

BC-SD:

BC amorphous solid dispersion

PVP:

Polyvinylpyrrolidone

Suc:

Sucrose fatty acid ester

PM:

Physical mixture

PXRD:

Powder X-ray diffraction

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Funding

This research was supported by Platform Project for Supporting Drug Discovery and Life Science Research (Basis for Supporting Innovative Drug Discovery and Life Science Research (BINDS)) from AMED under Grant Number JP20am0101084 and JP20am0101123.

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Authors

Contributions

KI designed the study as the first author, and drafted the manuscript. YN, SM, TI, and YK collected the test data. SO, SM, and YA helped in the interpretation of results. SN directed the research and reviewed the manuscript.

Corresponding author

Correspondence to Shinsaku Nakagawa.

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Conflict of interest

S. Otani and S. Maeda are employees of Mitsui Norin Co., Ltd. All other authors declare no competing interests.

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Ishimoto, K., Nakamura, Y., Otani, S. et al. Examination of dissolution ratio of β-carotene in water for practical application of β-carotene amorphous solid dispersion. J Food Sci Technol 59, 114–122 (2022). https://doi.org/10.1007/s13197-021-04991-z

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  • DOI: https://doi.org/10.1007/s13197-021-04991-z

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