Carotenoid particles and uses thereof

Abstract

This invention relates to the incorporation of bioactive cargo molecules into particles with carotenoids, such as lycopene. The incorporation of a cargo molecule into a carotenoid particle may for example increase the bioavailability of the cargo molecule in the bloodstream compared to other delivery systems. Carotenoid particles as described herein may be useful in the formulation of therapeutic and nutritional compounds for oral administration to individuals.

1 - 42 . (canceled) 
     
     
         43 . A population of particles, for example, micelles, reverse micelles or clusters thereof, each particle comprising a carotenoid compound and one or more cargo molecules. 
     
     
         44 . A population according to  claim 43 , wherein the carotenoid compound forms an outer, interim or cluster-bed layer which encapsulates an inner core or embedded or anchored structure, said core or structure comprising the cargo molecules in one or more particles, for example micelles, reverse micelles or clusters thereof in the population. 
     
     
         45 . A population according to  claim 43 , wherein the cargo molecules form an outer layer which encapsulates an inner core comprising the carotenoid compound in one or more particles, for example micelles, reverse micelles or clusters thereof in the population. 
     
     
         46 . A population according to  claim 44 , wherein the one or more particles form soluble micelles. 
     
     
         47 . A population according to  claim 46 , wherein at least 90% of the particles in the population are soluble micelles. 
     
     
         48 . A population according to  claim 43  which is one or more of the following:
 (i) in one or more particles, for example micelles, reverse micelles or clusters thereof, in the population, the carotenoid compound forms a matrix into which cargo molecules are anchored or embedded; 
 (ii) the carotenoid particles, for example micelles, reverse micelles or clusters thereof, comprise a single carotenoid compound; 
 (iii) the carotenoid particles, for example micelles, reverse micelles or clusters thereof comprise more than one carotenoid compound; 
 (iv) the carotenoid compound is lycopene; 
 (v) the carotenoid compound is lutein, zeaxanthin, canthaxanthin, phytoene, phytofluene, a xanthophyll, a carotene or any other carotenoid; 
 (vi) wherein the carotenoid compound is an extract, oleoresin, concentrate, or enriched or other product obtained from fruit, vegetable, plant, animal, fungus, yeast, or algae, or bacteria, or other source containing lycopene, or lutein, zeaxanthin, canthaxanthin, phytoene, phytofluene, or other xanthophylls, or carotenes, or any other carotenoids; or 
 (vii) each particle, for example micelle, reverse micelle or cluster thereof, in the population comprises 0.05 to 90% by weight of carotenoid compound. 
 
     
     
         49 . A population according to  claim 43  which is one or more of the following:
 (i) the cargo molecule is selected from the group consisting of whey protein, statin, isoflavone, and revestarol; or 
 (ii) the cargo molecule is a product of the fermentation, oxidation, processing, or degradation of food or a product of microbial metabolism; or 
 (iii) the cargo molecule is selected from the group consisting of food fermentation products, lecithin, phospholipids, carbohydrates, amino acids, flavones, flavonols, flavanones, flavanonols, isoflavones, catechins, gallocatechin, catechin 3-gallate, gallocatechin 3-gallate, epicatechins, epigallocatechin, epicatechin 3-gallate, flavon-3-ols, proanthocyanidins, anthocyanidins, aglycones of anthocyanins, silibinin, silymarin, curcuminoids, gingerols, ceramides; isoprene, prenol, isovaleric acid, geranyl pyrophosphate, eucalyptol, limonene, pinene, farnesyl pyrophosphate, artemisinin, bisabolol, geranylgeranyl pyrophosphate, retinol, retinal, phytol, taxol, forskolin, aphidicolin, squalene, lanosterol, terpenes, terpenoids, sterols and sterol esters, phytosterols, alpha-tocotrienols, beta-tocotrienols, gamma-tocotrienols, delta-tocotrienols, oils, shark or other cartilaginous fish oils, vegetable oils, oils from amaranth seed, oils from rice, oils from wheat germ, oils from olives, squalenes, retinoids, hydrolysable tannins, cinnamic acid, lignins polyphenols, vitamins, minerals, caffeine, theobromine, methy-Ixanthinesu, dimethyl-Ixanthinesu, para-Ixanthinesu, xanthine alkaloid, penicillins, fungal metabolites, cephalosporins, cardapenems, sulphonamides, quinolones, oxazodinones, macrolides, anti-viral drugs, cardiovascular drugs, metabolic drugs, anti-fungi drugs, anti-parasite drugs, and statins. 
 
     
     
         50 . A population according to  claim 43  which is one or more of the following:
 (i) the particles, micelles, reverse micelles or clusters thereof in said population do not contain whey protein; or 
 (ii) each particle, micelle, reverse micelle or cluster thereof in the population comprises 0.05 to 90% by weight of cargo molecule; or 
 (iii) the ratio of carotenoid compound to cargo molecule by weight is 0.02 or more; or 
 (iv) the ratio of carotenoid compound to cargo molecule by weight is up to 20; or 
 (v) the bioavailability of the cargo molecule after oral administration is increased by two fold or more by incorporation into the carotenoid particles, for example micelles, reverse micelles or clusters thereof; or 
 (vi) the carotenoid particle, for example a micelle, reverse micelle or cluster thereof, further comprises lecithin or other phospholipid; or 
 (vii) the ratio of carotenoid compound to cargo molecule by weight is up to 20 and the ratio of lecithin to carotenoid molecule in the carotenoid particle, for example micelle, reverse micelle or cluster thereof, by weight is 0.1 or more; or 
 (viii) the ratio of carotenoid compound to cargo molecule by weight is up to 20 and the ratio of lecithin to carotenoid molecule in the carotenoid particle, for example micelle, reverse micelle or cluster thereof, by weight is up to 1000; or 
 (ix) the carotenoid particles, for example micelles, reverse micelles or clusters thereof, are from 1 nm to 1 μm in size. 
 
     
     
         51 . A population according to  claim 43 , wherein the carotenoid particles, for example micelles, reverse micelles or clusters thereof, are obtainable by a method comprising:
 (a) dissolving the carotenoid compound in a first solvent to produce a first solution and the cargo molecule in a second solvent to produce a second solution,   (b) admixing the first and second solutions under conditions which allow the cargo molecule to incorporate into the matrix of the carotenoid, and   (c) evaporating and/or drying the admixture to produce carotenoid particles, for example micelles, reverse micelles or clusters thereof.   
     
     
         52 . A population according to  claim 43 , wherein the carotenoid particles, for example micelles, reverse micelles or clusters thereof, are obtainable by a method comprising:
 (a) dissolving the carotenoid compound in a first solvent to produce a first solution, and   (b) admixing the first solution with dried particles of the cargo molecules under conditions which allow the dried particles to incorporate in liquid carotenoid droplets.   
     
     
         53 . A population according to  claim 52  which is one or more of the following:
 (i) the admixture is evaporated and/or dried, or 
 (ii) the population is in the form of a solution, suspension or dry powder. 
 
     
     
         54 . A pharmaceutical or nutritional composition comprising a population of carotenoid particles, for example micelles, reverse micelles or clusters, thereof according to  claim 43  and an excipient. 
     
     
         55 . A composition according to  claim 54 , wherein the composition is formulated for oral administration. 
     
     
         56 . A method of producing a pharmaceutical or nutritional composition, the method comprising:
 admixing a population of carotenoid particles, for example micelles, reverse micelles or clusters thereof, according to  claim 43  with one or more carriers, vehicles and/or excipients.   
     
     
         57 . A method of improving the delivery of a cargo molecule to a target tissue which expresses carotenoid receptors, the method comprising:
 (a) incorporating the cargo molecule into a population of carotenoid particles, for example micelles, reverse micelles or clusters thereof, according to  claim 43 , and   (b) administering the population of carotenoid particles to an individual.   
     
     
         58 . A method according to  claim 55 , wherein the target tissue which expresses carotenoid receptors is one or more of liver, testis, prostate, lymph tissue, or adrenal gland. 
     
     
         59 . A method of treatment comprising administering a population of particles, for example micelles, reverse micelles or clusters thereof, according to  claim 43  to an individual in need thereof. 
     
     
         60 . A method according to  claim 59 , wherein the individual has a condition which is ameliorated by the cargo molecule, and one or more of the following:
 (i) the cargo molecule is whey protein and the condition is  Chlamydia  infection or elevated serum cholesterol levels; or   (ii) the cargo molecule is statin and the condition is selected from the group consisting of cardiovascular disease, dementia, hypertension, cancer, cataract, and elevated serum cholesterol levels; or   (iii) the cargo molecule is resveratrol and the condition is selected from the group consisting of elevated cholesterol and/or triglycerides, diabetes, cardiovascular or cerebrovascular disease, cancer, acute or chronic bacterial infections, acute or chronic fungal infections, acute or chronic viral infections, neurodegenerative diseases, gastrointestinal tract disease, connective tissue disease, arthritis, and inflammatory conditions; or   (iv) the cargo molecule is an isoflavone and the condition is selected from the group consisting of elevated cholesterol and/or triglycerides, diabetes, cardiovascular or cerebrovascular disease, cancer, neurodegenerative diseases, connective tissue disease, and inflammatory conditions.