Phytosterols are sterols naturally occurring in plant cells and well known for their cholesterollowering activity, as witnessed by the large number of food supplements based on these functional ingredients available on the market. However, the marked hydrophobic character of phytosterols makes their solubility in biological fluids extremely low, with disadvantageous consequences on the bioavailability and therapeutic efficacy. In this work, we explore the effect of particle size reduction on the water solubility of stigmasterol, one of the most abundant phytosterols, through the formulation of nanocystals. A robust, top-down production process was employed to prepare stigmasterol nanocrystals, subsequently characterized by thermal and spectroscopic techniques. When formulated as nanocrystals, the solubility of stigmasterol in water and in simulated gastro-intestinal fluids was boosted compared to the raw material. The increased solubility of stigmasterol nanocrystals makes such formulation a promising candidate for the development of medicinal/nutraceutical products with enhanced bioavailability.

Nanocrystals as Tool to Enhance Stigmasterol Oral Bioavailability

Pireddu, Rosa
Membro del Collaboration Group
;
Sinico, Chiara
Membro del Collaboration Group
;
Ennas, Guido
Membro del Collaboration Group
;
Valenti, Donatella
Membro del Collaboration Group
;
Marongiu, Francesca
Membro del Collaboration Group
;
Maria Fadda, Anna
Membro del Collaboration Group
;
Schlich, Michele
Membro del Collaboration Group
;
Lai, Francesco
Membro del Collaboration Group
2021-01-01

Abstract

Phytosterols are sterols naturally occurring in plant cells and well known for their cholesterollowering activity, as witnessed by the large number of food supplements based on these functional ingredients available on the market. However, the marked hydrophobic character of phytosterols makes their solubility in biological fluids extremely low, with disadvantageous consequences on the bioavailability and therapeutic efficacy. In this work, we explore the effect of particle size reduction on the water solubility of stigmasterol, one of the most abundant phytosterols, through the formulation of nanocystals. A robust, top-down production process was employed to prepare stigmasterol nanocrystals, subsequently characterized by thermal and spectroscopic techniques. When formulated as nanocrystals, the solubility of stigmasterol in water and in simulated gastro-intestinal fluids was boosted compared to the raw material. The increased solubility of stigmasterol nanocrystals makes such formulation a promising candidate for the development of medicinal/nutraceutical products with enhanced bioavailability.
2021
Biological Availability; Solubility; Stigmasterol; Nanoparticles; Phytosterols
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11584/326453
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