LIPID COMPOSITION COMPRISING ANTIOXIDANTS AND NATURAL POLYPHENOLS AS A NON-PHARMACOLOGICAL ALTERNATIVE FOR THE TREATMENT AND PREVENTION OF NON-ALCOHOLIC FATTY LIVER DISEASE (NAFLD)

Abstract

The present application provides lipid-based compositions comprising bioactives of natural origin. In particular, the compositions disclosed herein comprise antioxidants, such as anthocyanins, polyphenols, such as curcuminoids, mixtures of omega-3 and omega-7 unsaturated fatty acids, phospholipids, liposoluble vitamins and medium chain triglycerides, which provide a non-pharmacological alternative for the treatment and prevention of liver diseases related to non-alcoholic fatty liver disease (NAFLD).

Claims

1. A lipid-based composition comprising bioactives agents of natural origin, wherein said bioactive agents include cyanidin-3-glucoside as an antioxidant, one or more polyphenols, a phospholipid, a mixture of at least two omega-3 fatty acids, a mixture of medium chain triglycerides (MCT), at least one fat-soluble vitamin, and an omega-7 fatty acid.

2. The composition of claim 1, wherein the cyanidin-3-glucoside is an anthocyanin obtained from Chilean Maqui, Aristotelia chilensis.

3. The composition of claim 1, wherein the polyphenols comprise a mixture of curcuminoids.

4. The composition of claim 1, wherein the mixture of omega-3 fatty acids comprises a mixture of DHA/EPA with a ratio of 2:1, respectively.

5. The composition of claim 1, wherein the phospholipid is selected from at least one of phosphatidylcholine, phosphatidylserine, sphingomyelin or phytosphingosine.

6. The composition of claim 1, wherein the fat-soluble vitamin is vitamin D3, vitamin E or a mixture thereof.

7. The composition of claim 1, wherein the mixture of MCT comprises glycerol esters of fatty acids of between 8 and 10 carbon atoms.

8. A food product, nutraceutical, dietary supplement, food supplement, special diet foods, or foods for special medical purposes, comprising a composition according to claim 1.

9. A method for treating non-alcoholic fatty liver disease (NAFLD) comprising orally administering to an individual in need thereof an effective amount of a composition according to claim 1.

10. The method of claim 9, wherein the administration of the composition is daily.

11. Use of the composition according to claim 1, to prevent or reduce infiltration of lipids in a liver.

12. Use of the composition according to claim 1, to improve insulin sensitivity in an individual who requires it.

13. Use of the composition according to claim 1, to improve at least one of anthropometric, hemodynamic or biochemical parameters related to non-alcoholic fatty liver disease (NAFLD).

14. Use of the composition according to claim 1, for the preparation of a medicament useful in the treatment or prevention of a liver disease.

15. The use according to claim 14, wherein the liver disease is non-alcoholic fatty liver disease (NAFLD).

Description

DETAILED DESCRIPTION OF THE INVENTION

[0031] Detailed embodiments of the present invention are described below in the present document; however, it should be understood that they are merely illustrative and can be incorporated in various forms. In addition, each of the examples given in relation to the various embodiments of the invention are intended to be illustrative and not restrictive.

[0032] The present invention relates to a lipid-based composition with bioactives of natural origin. In a preferred embodiment, the lipid-based composition comprising antioxidants and polyphenols of natural origin.

[0033] In a particular embodiment of the invention, the composition comprises a mixture of lipids of natural origin. In a preferred embodiment of the invention, the lipids of natural origin provide bioactive agents among which are at least a phospholipid, omega-3 and omega-7 fatty acids, medium chain triglycerides (MTCs), fat-soluble vitamins, antioxidants and polyphenols.

[0034] In a preferred embodiment, the lipid-based composition of the invention comprises at least one antioxidant of natural origin in a range of between about 1.0 to about 3.0 weight percent. In another embodiment, the lipid-based composition of the invention includes at least one antioxidant in a range of 2.0 to 2.5 weight percent.

[0035] In still other embodiments, the antioxidant of natural origin included in the lipid-based composition of the invention is of the anthocyanin family. In a preferred embodiment, said anthocyanin is cyanidin-3-glucoside (C3G), also called chrysanthamine.

[0036] In a particular embodiment, the anthocyanins present in the composition of the invention are obtained from dark colored fruits and vegetables. In a still more preferred embodiment, cyanidin-3-glucoside is obtained from the Chilean maqui, Aristotelia chilensis.

[0037] In another embodiment, the invention relates to a lipid-based composition with bioactive agents comprising at least one polyphenol of natural origin, wherein the at least one polyphenol is in a range from about 0.4 to about 1.0 weight percent. In a preferred embodiment the at least one polyphenol is between about 0.5 to about 0.8 weight percent.

[0038] In a preferred embodiment, at least one polyphenol found in the lipid-based composition of the invention is obtained from turmeric, that is, it corresponds to a curcuminoid or to a mixture thereof. In a further embodiment, the polyphenol of natural origin present in the composition of the invention comprises one or more curcuminoids selected from a group including, but not limited to, curcumin, demethoxycurcumin and bisdemethoxyurcumin.

[0039] In one embodiment, the lipid-based composition with bioactive agents of the invention includes a mixture of two or more omega-3 unsaturated fatty acids. In a preferred embodiment, the omega-3 unsaturated fatty acids are selected from a group comprising docosahexaenoic acid (DHA), Eicosapentaenoic acid (EPA), and α-linolenic acid (ALA).

[0040] In a preferred embodiment, the lipid-based composition of the invention includes a mixture of DHA and EPA. In an even more preferred embodiment, the composition of the invention comprises from about 14 to about 25% of DHA and from about 7 to about 13% of EPA. In still another preferred embodiment, the mixture comprises DHA and EPA in a ratio of 2:1, respectively.

[0041] In a preferred embodiment, the lipid-based composition with bioactives of the invention includes from about 14 to about 23 weight percent of a phospholipid, more preferably from about 17 to about 21 weight percent.

[0042] In a particular embodiment, the lipid-based composition of the invention comprises a phospholipid selected from a group including, but not limited to, phosphatidylcholine, phosphatidylserine, sphingomyelin and/or phytosphingosine. In an even more preferred embodiment, the phospholipid is phosphatidylcholine.

[0043] In a preferred embodiment, the phospholipid is obtained from natural sources including, but not limited to, soy lecithin.

[0044] In one embodiment, the lipid-based composition with bioactives of the invention comprises a mixture of medium chain triglycerides (MCTs) in a range of between about 38 to about 55 weight percent. In other embodiments, the MTCs are in a range from about 45 to about 50 weight percent.

[0045] In one embodiment, the mixture of MTCs included in the lipid-based composition of the invention, comprises esters of glycerol fatty acids of 8 to 10 carbon atoms. In an even more preferred embodiment, the MTCs are glycerol esters of caprylic and capric acid mixtures.

[0046] In a further embodiment, the lipid-based composition with bioactives of the invention comprises at least one fat-soluble vitamin in a range from about 1.0×10.sup.−4 to about 3.0×10.sup.−4 percent by weight. In other embodiments, the composition of the invention includes at least one fat-soluble vitamin in a range from about 1.5×10.sup.−4 to about 2.5×10.sup.−4 percent by weight.

[0047] In a preferred embodiment, the lipid base composition of the invention comprises at least one fat-soluble vitamin selected from a group consisting of vitamin D3, vitamin E, and mixtures thereof.

[0048] In one embodiment, the lipid-based composition with bioactive agents of the invention comprises at least one omega-7 unsaturated fatty acid in a range from about 5 to about 15 weight percent. In another embodiment, the composition comprises at least one omega-7 unsaturated fatty acid in a range of between about 6 to about 10 weight percent.

[0049] In one embodiment, the at least one omega-7 unsaturated fatty acid comprises palmitoleic acid. In a preferred embodiment, palmitoleic acid is obtained from buckthorn oil.

[0050] In one embodiment, the lipid-based composition of the invention is in a form suitable for direct consumption, such as in the form of encapsulation, liquid emulsion, microencapsulated powder or a suspension.

[0051] In another embodiment, the lipid-based composition of the invention can be incorporated into different matrices commonly employed in the food industry, such as powdered or ready-to-eat beverages, smoothies, creams, cookies, bakery products, snacks, beverages and dairy products.

[0052] In some embodiments, the lipid-based composition of the invention is provided as a gel, dispersion, suspension or solution in oil.

[0053] In some embodiments, the use of the lipid-based composition of the invention directly influences the pathophysiological mechanisms of NAFLD. In other embodiments the use of the composition of the invention improves insulin sensitivity, reduces adipose tissue inflammation and hepatic inflammation and slows liver fibrosis.

[0054] In another embodiment the use of the lipid-based composition of the invention improves the infiltration of lipids in the liver, as do the anthropometric, hemodynamic and/or biochemical parameters related to NAFLD.

[0055] In another embodiment, the application provides a method for treating or preventing NAFLD in individuals suffering from said disease or at risk of developing it. In a preferred embodiment, the application relates to a method of treatment comprising orally administering daily a therapeutically effective amount of a composition according to any of the modalities described herein to the individual in need thereof.

[0056] In said embodiments, the effective amount of the composition is based, at least in part, on the weight of the human being who needs it.

EXAMPLES

[0057] The following examples are intended to illustrate the invention and should not be construed as limiting the invention in any way.

Example 1

[0058] Lipid based compositions were prepared from natural ingredients, the content of which is shown in Table 1:

TABLE-US-00001 TABLE 1 Exemplary compositions of the invention Source % in weigh Soy lecithin 14-21 DHA 14-25 EPA  7-13 Caprylic and capric acid triglycerides 38-55 Chilean Maqui powder 1-3 Vitamin D3 0.0001-0.0003 Buckthorn oil  6-10 Tumeric 0.4-0.8

[0059] The daily administration of the lipid-based composition comprising bioactives of natural origin has the ability to improve the physiopathological phenomena associated with the development of liver diseases such as NAFLD.

[0060] Thus, the lipid-based composition developed by the inventors offers an effective non-pharmacological alternative for the treatment of patients suffering from these diseases or at risk of developing them.