Carotenoids of enhanced bioavailability
View Patent ↗Carotenoid compositions of enhanced solubility and bioavailability are described that contain at least one carotenoid with at least one solubility-enhancing polymer. In one embodiment, the carotenoid is a provitamin A carotenoid such as β-carotene. In another embodiment the carotenoid is a non-provitamin A carotenoid such as lycopene or lutein. Described methods to produce the bioenhanced products include dry blending and solvent spray drying. In accordance with certain embodiments of the invention, the method includes the steps of providing a mixture comprising the carotenoid, a solubility-enhancing polymer and a solvent and removing the solvent to produce an amorphous form of the carotenoid. Products made by the invention's compositions and methods include pharmaceuticals, nutraceuticals, cosmetic, and personal care products for man and animal.
1. A composition comprising a solid solution wherein the solid solution comprises one or more carotenoid(s) and one or more solubility-enhancing polymer(s) wherein said carotenoid is substantially amorphous and exhibits enhanced bioavailability compared to a control composition without the solubility-enhancing polymer, and wherein the polymer is selected from the group consisting of polyvinylpyrrolidone, hydroxypropylcellulose, hydroxypropylmethylcellulose, hydroxypropylmethylcellulose acetate succinate, hydroxypropylmethylcellulose phthalate and mixtures thereof.
2. The composition of claim 1 wherein said carotenoid is completely amorphous.
3. The composition of claim 1 wherein the ratio of carotenoid to solubility-enhancing polymer is between about 25% carotenoid: 75% polymer to about 75% carotenoid: 25% polymer.
4. The composition of claim 1 wherein the composition comprises spray dried particles of carotenoid and polymer.
5. The composition of claim 4 wherein the spray dried particles of carotenoid and polymer have an average particle size of from about 0.5 μm-500 μm.
6. The composition of claim 1 wherein the carotenoid comprises a provitamin A carotenoid.
7. The composition of claim 6 wherein the provitamin A carotenoid is selected from the group consisting of α-carotene, β-carotene, β-cryptoxanthin, and mixtures thereof.
8. The composition of claim 1 wherein the carotenoid comprises a non-provitamin A carotenoid.
9. The composition of claim 8 wherein the non-provitamin A carotenoid is selected from the group consisting of lycopene, lutein, zeaxanthin, and mixtures thereof.
10. A dosage form comprising the composition of claim 1 .
11. The dosage form of claim 10 wherein the dosage form comprises an oral, solid-dosage form.
12. The dosage form of claim 11 wherein the dosage form provides at least one of:
a) a maximum plasma concentration for an active form of carotenoid that is at least 1.25 times greater than that of a control composition containing crystalline carotenoid;
b) an increase in the exposure (AUC 0-24h ) of at least 1.25 times that of a control composition containing crystalline carotenoid.