Sustained release of nutrients
Nutritional compositions delivered in vivo in a time controlled manner sustainable over long periods of time, provide enhancing athletic performance, increased hand/eye coordination and concentration on the task at hand.
1. A composition for in vivo consumption, comprising:
an aqueous suspension, comprising
(a) one or more nutritional supplements; and,
(b) one or more hydrogel microparticles that encapsulate one or more nutritional supplements of (a), wherein the one or more hydrogel microparticles
(i) have a diameter between 1 to 1000 micrometers;
(ii) comprise one or more compounds that are non-toxic, crosslinked, and that release the encapsulated one or more nutritional supplements in a time controlled and sustained manner in vivo;
(iii) are pH-sensitive, wherein one or more compounds of the hydrogel microparticles do not swell at pH 1-3; and
(iv) are temperature-sensitive, wherein one or more compounds of the hydrogel microparticles have a lower critical solution temperature in aqueous solution.
2. The composition of claim 1 , wherein the one or more nutritional supplements are selected from the group consisting of: minerals, proteins, carbohydrates, amino acids, lipids, electrolytes and vitamins.
3. The composition of claim 1 , wherein the one or more compounds in (b)(ii) for the time controlled and sustained release of the nutritional supplements comprise biodegradable polymers, bioadhesives and/or binders.
4. The composition of claim 3 , wherein the biodegradable polymers and binders comprise one or more of poly(lactide)s, poly(glycolide)s, poly(lactide-co-glycolide)s, poly(lactic acid)s, poly(glycolic acid)s, poly(lactic acid-co-glycolic acid)s, polycaprolactone, polycarbonates, polyesteramides, polyanhydrides, poly(amino acids), polyorthoesters, polyacetyls, polycyanoacrylates, polyetheresters, poly(dioxanone)s, poly(alkylene alkylate)s, copolymers of polyethylene glycol and polyorthoester, biodegradable polyurethanes, polysaccharides and polysaccharide copolymers with polyethers.
5. The composition of claim 1 , wherein the nutritional supplements are in a concentration and released in vivo, in a time controlled and sustained release to increase exercise duration and cumulative power output potential by at least about 1% to about 50%, about 50% to about 100%, about 100% to about 500% or about 500% to about 1000% when compared to a control with no nutritional supplement ingestion pre and during exercise.
6. The composition of claim 1 , wherein the nutritional supplements are in a concentration and released in vivo, in a time controlled and sustained release to increase burst energy duration and power output by at least about 1% to about 50%, about 50% to about 100%, about 100% to about 500% or about 500% to about 1000% when compared to a control with no nutritional supplement ingestion pre and during exercise.
7. The composition of claim 1 , wherein the nutritional supplements are in a concentration and released in vivo, in a time controlled and sustained release to increase the number of effective burst events by at least about 1% to about 50%, about 50% to about 100%, about 100% to about 500% or about 500% to about 1000% when compared to a control with no nutritional supplement ingestion pre and during exercise.
8. The composition of claim 1 , wherein the nutritional supplements are in a concentration and released in vivo, in a time controlled and sustained release to decrease the duration of recovery time between burst events by at least about 1% to about 50%, about 50% to about 100%, about 100% to about 500% or about 500% to about 1000% when compared to a control with no nutritional supplement ingestion pre and during exercise.
9. The composition of claim 1 , wherein the nutritional supplements are in a concentration and released in vivo, in a time controlled and sustained release increase continuous exercise power output by about 1% to about 50%, about 50% to about 100%, about 100% to about 500% or about 500% to about 1000%, advantageously about 1% to about 50% at about VO 2 62% and about 1% to about 25% increase in high intensity exercise at about VO 2 86%, and increase the number of effective burst periods by about 1% to about 50%, about 50% to about 100%, about 100% to about 500% or about 500% to about 1000% as compared to performance when utilizing commercially available performance enhancing drinks.
10. The composition of claim 1 , wherein the one or more compounds in (b)(ii) for time controlled and sustained release of the nutritional supplements in vivo release the nutritional supplements in effective amounts and concentrations over sustained periods of time to increase exercise duration and cumulative power output potential by at least a about 1% to about 50%, about 50% to about 100%, about 100% to about 500% or about 500% to about 1000%, increase burst energy duration and power output by at least about 1% to about 50%, about 50% to about 100%, about 100% to about 500% or about 500% to about 1000%, increase the number of effective burst events from about 1% to about 50%, about 50% to about 100%, about 100% to about 500% or about 500% to about 1000%, decreases the duration of recovery time between burst events by at least about 1% to about 50%, about 50% to about 100%, about 100% to about 500% or about 500% to about 1000%, when compared to a control with no nutritional supplement ingestion pre and during exercise.
11. The composition of claim 1 , wherein the one or more compounds in (b)(ii) for time controlled and sustained release of the nutritional supplements in vivo release the nutritional supplements in effective amounts and concentrations over sustained periods of time to increase continuous exercise power output by about 1% to about 50%, about 50% to about 100%, about 100% to about 500% or about 500% to about 1000%, advantageously about 1% to about 50% at about VO 2 62% and about 1% to about 25% increase in high intensity exercise at about VO 2 86%, and increase the number of effective burst periods by at least about 100% as compared to performance when utilizing commercially available performance enhancing drinks.
12. The composition of claim 1 , wherein the composition is a beverage, a gum, or a food snack.
13. The composition of claim 1 , wherein the one or more hydrogel microparticles comprise at least one modified polysaccharide.
14. The composition of claim 13 , wherein the at least one modified polysaccharide comprises a modification selected from the group consisting of: carboxylic acid, acryloyl or methacryloyl, hydroxyalkyl, ester, grafted fatty acid moieties, oligo(alkylene oxide) grafts, functionalized hydrophobes, grafted amphiphiles, or side chain derivatizations to introduce aldehydic or carboxylic groups.
15. The composition of claim 14 , wherein the functionalized hydrophobe is cholesterol.
16. The composition of claim 14 , wherein the grafted amphiphile is alkenylsuccinate.
17. The composition of claim 14 , wherein the polysaccharide is modified with oligo(alkylene oxide) grafts.
18. The composition of claim 1 , wherein the one or more hydrogel microparticles increase the retention time of nutrients in the small intestine because of the mucoadhesive nature of the one or more hydrogel microparticles.
19. The composition of claim 1 , wherein the crosslinking is performed using inorganic salts, or free radical initiators, or redox systems involving ascorbic acid, or a naturally occurring crosslinker.
20. The composition of claim 19 , wherein the crosslinking is ionic crosslinking.
21. The composition of claim 20 , wherein the ionic crosslinking is with an anionic polysaccharide.
22. The composition of claim 1 , wherein the one or more compounds of (b)(ii) for time controlled and sustained release are covalently crosslinked.
23. The composition of claim 1 , wherein the one or more temperature-sensitive hydrogel microparticles are swollen by water and disperse upon cooling the composition below the lower critical solution temperature of the one or more compounds of (b)(ii).
24. The composition of claim 1 , wherein the one or more temperature-sensitive hydrogel microparticles comprise hydroxypropyl cellulose.
25. The composition of claim 23 , wherein the one or more temperature-sensitive hydrogel microparticles comprise hydroxypropyl cellulose.
26. The composition of claim 1 , wherein the one or more pH-sensitive hydrogel microparticles swell in the pH environment of the small intestine.
27. The composition of claim 26 , wherein the release rate of the one or more nutritional supplements from the one or more pH-sensitive hydrogel microparticles is increased in the small intestine relative to that in the stomach.
28. The composition of claim 1 , wherein the one or more pH-sensitive hydrogel microparticles comprise alginate.
29. The composition of claim 1 , wherein the release rate of the one or more nutritional supplements from the one or more temperature-sensitive and pH-sensitive hydrogel microparticles is increased in the small intestine relative to that in the stomach.
30. The composition of claim 1 , wherein the one or more temperature-sensitive and pH-sensitive hydrogel microparticles comprise hydroxypropyl cellulose and alginate.
31. The composition of claim 1 , wherein the one or more compounds of (b)(ii) for time controlled and sustained release comprise a polysaccharide, wherein the polysaccharide is a naturally occurring anionic polymer.
32. The composition of claim 1 , wherein the composition comprises a surfactant.
33. The composition of claim 1 , wherein the lower critical solution temperature in (b)(iv) is at least about 32° C.
34. A method of improving athletic performance and endurance comprising
administering to an individual a composition of claim 1 , wherein the one or more nutritional supplements are selected from the group consisting of: minerals, proteins, lipids, vitamins, carbohydrates, amino acids, and electrolytes; and,
consuming the composition wherein the one or more compounds in (b)(ii) for sustained release of the nutritional supplements in vivo release the nutritional supplements in effective amounts and concentrations over extended periods of time to increase exercise duration and cumulative power output potential by at least about 1% to about 50%, about 50% to about 100%, about 100% to about 500% or about 500% to about 1000%, increase burst energy duration and power output by at least about 1% to about 50%, about 50% to about 100%, about 100% to about 500% or about 500% to about 1000%, increase the number of effective burst events from about 1% to about 50%, about 50% to about 100%, about 100% to about 500% or about 500% to about 1000%, decreases the duration of recovery time between burst events by at least about 1% to about 50%, about 50% to about 100%, about 100% to about 500% or about 500% to about 1000%, when compared to a control with no nutritional supplement ingestion pre and during exercise; and,
improving athletic performance and endurance.
35. A composition for in vivo consumption, comprising:
an aqueous suspension, comprising
(a) one or more nutritional supplements; and,
(b) one or more hydrogel microparticles that encapsulate one or more nutritional supplements of (a), wherein the one or more hydrogel microparticles
(i) have a diameter between 1 to 1000 micrometers;
(ii) comprise one or more compounds that are non-toxic, crosslinked, and that release the encapsulated one or more nutritional supplements in a time controlled and sustained manner in vivo, wherein at least one of the compounds is selected from the group consisting of: poly(lactide)s, poly(glycolide)s, poly(lactide-co-glycolide)s, poly(lactic acid)s, poly(glycolic acid)s, poly(lactic acid-co-glycolic acid)s, polycaprolactone, polycarbonates, polyesteramides, polyanhydrides, poly(amino acids), polyorthoesters, polyacetyls, polycyanoacrylates, polyetheresters, poly(dioxanone)s, poly(alkylene alkylate)s, copolymers of polyethylene glycol and polyorthoester, biodegradable polyurethanes, polysaccharides and polysaccharide copolymers with polyethers;
(iii) are pH-sensitive, wherein one or more compounds of the hydrogel microparticles do not swell at pH 1-3; and
(iv) are temperature-sensitive, wherein one or more compounds of the hydrogel microparticles have a lower critical solution temperature in aqueous solution.