COMPOSITIONS COMPRISING LIPID DROPLETS ENCAPSULATED WITHIN POLYSACCHARIDE WALLS AND USES THEREOF
Drug delivery systems are needed to assist in improving the therapeutic characteristics of pharmaceutical agents. Provided is a dry composition, comprising a polysaccharide, such as inulin, and lipid droplets, wherein the lipid droplets are encapsulated within polymeric chains of the polysaccharide, and wherein the polysaccharide is not in a nano-particulate form. The use of such compositions enables efficient delivery of agents, such as poorly-water soluble drugs and antibiotics.
1 . A dry composition comprising:
(i) a polysaccharide; and
(ii) lipid droplets,
wherein the lipid droplets are encapsulated within polymeric chains of the polysaccharide, and wherein the polysaccharide is not in a nano-particulate form.
2 . The composition of claim 1 , wherein the polysaccharide is a dietary polysaccharide.
3 . The composition of claim 2 , wherein the polysaccharide is selected from the group consisting of inulin, cellulose and glucomannan.
4 . The composition of claim 3 , wherein the polysaccharide is inulin.
5 . The composition of any one of claims 1 to 4 , wherein the lipid droplets comprise a medium chain length fatty acid.
6 . The composition of any one of claims 1 to 5 , wherein the ratio of polysaccharide to lipid in the composition ranges from about 10:90 to about 90:10.
7 . The composition of claim 6 , wherein the ratio of polysaccharide to lipid in the composition ranges from about 50:50 to about 75:25.
8 . The composition of claim 4 , wherein the composition is used for improving the health of a subject.
9 . The composition of claim 8 , wherein the gastrointestinal health of the subject is improved.
10 . The composition of any one of claims 1 to 9 , further comprising an active substance, wherein the active substance is contained within the lipid droplets.
11 . The composition of claim 10 , wherein the active substance is an agent that can dissolve in the lipid droplets.
12 . The composition of claim 10 or claim 11 , wherein the active substance is a pharmaceutical agent.
13 . The composition of claim 12 , wherein the pharmaceutical agent is a poorly water-soluble drug.
14 . The composition of claim 12 or claim 13 , wherein the pharmaceutical agent is selected from the group consisting of an antimicrobial agent, an anti-inflammatory agent, an anti-histamine, a cholesterol-lowering drug, or a psychotropic drug.
15 . The composition of claim 14 , wherein the antimicrobial agent is one or more of an antibiotic, an antimicrobial peptide, and an antifungal agent.
16 . The composition of claim 15 , wherein the antibiotic is selected from the group consisting of rifampicin, tobramycin and vancomycin.
17 . The composition of claim 14 , wherein the cholesterol-lowering drug is a statin or fenofibrate.
18 . The composition of claim 17 , wherein the statin is simvastatin.
19 . The composition of claim 14 , wherein the psychotropic drug is lurasidone.
20 . The composition of any one of claim 1 to 19 , further comprising an excipient or stabilizer.
21 . The composition of claim 20 , wherein the stabilizer is lecithin.
22 . The composition of any one of claims 1 to 21 , wherein the composition is formulated for oral delivery.
23 . The composition of any one of claims 1 to 21 , wherein the composition is produced by a method comprising:
(i) producing a lipid-in-water nano-emulsion comprising the lipid droplets and the polysaccharide, wherein the polysaccharide is dissolved in the aqueous phase of the nano-emulsion; and
(ii) spray-drying the nano-emulsion.
24 . The composition of claim 23 , wherein the nano-emulsion is produced by homogenizing a mixture comprising the lipid droplets and adding the polysaccharide in aqueous form to the mixture.
25 . The composition of any one of claims 1 to 24 , wherein the microparticles have an average diameter of <15 μm.
26 . A method for improving the health of a subject, or for treating or preventing a disease or disorder in a subject, the method comprising administering the composition of any one of claims 4 to 25 to the subject.
27 . The method of claim 26 , wherein the gastrointestinal health of the subject is improved.
28 . The method of claim 26 , wherein a metabolic disease or disorder is treated or prevented in the subject.
29 . A method for treating or preventing a microbial infection is a subject, the method comprising administering the composition of any one of claims 12 to 25 to the subject, wherein the pharmaceutical agent is an antimicrobial agent.
30 . The method of claim 29 , wherein the microbial infection is a bacterial infection.
31 . The method of claim 30 , wherein the bacterial infection is due to Staphylococcus aureus.
32 . The method of claim 30 or claim 31 , wherein the bacterial infection forms part of a biofilm.
33 . A method for administering an active substance to a subject, wherein the method comprises administering to the subject a composition of any one of claims 10 to 25 .
34 . A method for producing a composition of any one of claims 1 to 33 , wherein the method comprises spray-drying a lipid-in-water nano-emulsion comprising the lipid droplets and the polysaccharide.
35 . A dry composition comprising:
(i) a polysaccharide;
(ii) lipid droplets; and
(iii) an excipient or stabilizer,
wherein the lipid droplets are encapsulated within polymeric chains of the polysaccharide, and wherein the polysaccharide is not in a nano-particulate form.
36 . The composition of claim 35 , wherein the polysaccharide is a dietary polysaccharide.
37 . The composition of claim 36 , wherein the polysaccharide is selected from the group consisting of inulin, cellulose and glucomannan.
38 . The composition of claim 37 , wherein the polysaccharide is inulin.
39 . The composition of any one of claims 35 to 38 , wherein the lipid droplets comprise a medium chain length fatty acid.
40 . The composition of any one of claims 35 to 39 , wherein the ratio of polysaccharide to lipid in the composition ranges from about 10:90 to about 90:10.
41 . The composition of claim 40 , wherein the ratio of polysaccharide to lipid in the composition ranges from about 50:50 to about 75:25.
42 . The composition of any one of claims 35 to 41 , wherein the stabilizer is lecithin.
43 . The composition of any one of claims 38 to 42 , wherein the composition is used for improving the health of a subject.
44 . The composition of claim 43 , wherein the gastrointestinal health of the subject is improved.
45 . The composition of any one of claims 35 to 44 , further comprising an active substance, wherein the active substance is contained within the lipid droplets.
46 . The composition of claim 45 , wherein the active substance is an agent that can dissolve in the lipid droplets.
47 . The composition of claim 45 or claim 46 , wherein the active substance is a pharmaceutical agent.
48 . The composition of claim 47 , wherein the pharmaceutical agent is a poorly water-soluble drug.
49 . The composition of claim 47 or claim 48 , wherein the pharmaceutical agent is selected from the group consisting of an antimicrobial agent, an anti-inflammatory agent, an anti-histamine, a cholesterol-lowering drug, or a psychotropic drug.
50 . The composition of claim 49 , wherein the antimicrobial agent is one or more of an antibiotic, an antimicrobial peptide, and an antifungal agent.
51 . The composition of claim 50 , wherein the antibiotic is selected from the group consisting of rifampicin, tobramycin and vancomycin.
52 . The composition of claim 49 , wherein the cholesterol-lowering drug is a statin or fenofibrate.
53 . The composition of claim 52 , wherein the statin is simvastatin.
54 . The composition of claim 49 , wherein the psychotropic drug is lurasidone.
55 . The composition of any one of claims 35 to 54 , wherein the composition is produced by a method comprising:
(i) producing a lipid-in-water nano-emulsion comprising the lipid droplets, the polysaccharide, and the excipient or stabilizer, wherein the polysaccharide is dissolved in the aqueous phase of the nano-emulsion; and
(ii) spray-drying the nano-emulsion.
56 . The composition of claim 55 , wherein the nano-emulsion is produced by homogenizing a mixture comprising the lipid droplets and the excipient or stabilizer, and adding the polysaccharide in aqueous form to the mixture.
57 . The composition of any one of claims 35 to 56 , wherein the microparticles have an average diameter of <15 μm.
58 . A method for improving the health of a subject, or for treating or preventing a disease or disorder in a subject, the method comprising administering the composition of any one of claims 38 to 57 to the subject.
59 . The method of claim 58 , wherein the gastrointestinal health of the subject is improved.
60 . The method of claim 58 , wherein a metabolic disease or disorder is treated or prevented in the subject.
61 . A method for treating or preventing a microbial infection is a subject, the method comprising administering the composition of any one of claims 47 to 57 to the subject, wherein the pharmaceutical agent is an antimicrobial agent.
62 . The method of claim 61 , wherein the microbial infection is a bacterial infection.
63 . The method of claim 62 , wherein the bacterial infection is due to Staphylococcus aureus.
64 . The method of claim 62 or claim 63 , wherein the bacterial infection forms part of a biofilm.
65 . A method for administering an active substance to a subject, wherein the method comprises administering to the subject a composition of any one of claims 45 to 57 .
66 . A method for producing a composition of any one of claims 35 to 57 , wherein the method comprises spray-drying a lipid-in-water nano-emulsion comprising the lipid droplets, the polysaccharide, and the excipient or stabilizer.
67 . A dry composition comprising:
(i) inulin;
(ii) an active substance; and
(iii) lipid droplets,
wherein the lipid droplets are encapsulated within polymeric chains of inulin, and wherein the polysaccharide is not in a nano-particulate form.
68 . The composition of claim 67 , wherein the lipid droplets comprise a medium chain length fatty acid.
69 . The composition of claim 67 or claim 68 , wherein the ratio of inulin to lipid in the composition ranges from about 10:90 to about 90:10.
70 . The composition of claim 69 , wherein the ratio of inulin to lipid in the composition ranges from about 50:50 to about 75:25.
71 . The composition of any one of claims 67 to 70 , wherein the active substance is contained within the lipid droplets.
72 . The composition of claim 71 , wherein the active substance is an agent that can dissolve in the lipid droplets.
73 . The composition of any one of claims 67 to 72 , wherein the active substance is a pharmaceutical agent.
74 . The composition of claim 73 , wherein the pharmaceutical agent is a poorly water-soluble drug.
75 . The composition of claim 73 or claim 74 , wherein the pharmaceutical agent is selected from the group consisting of an antimicrobial agent, an anti-inflammatory agent, an anti-histamine, a cholesterol-lowering drug, or a psychotropic drug.
76 . The composition of claim 75 , wherein the antimicrobial agent is one or more of an antibiotic, an antimicrobial peptide, and an antifungal agent.
77 . The composition of claim 76 , wherein the antibiotic is selected from the group consisting of rifampicin, tobramycin and vancomycin.
78 . The composition of claim 75 , wherein the cholesterol-lowering drug is a statin or fenofibrate.
79 . The composition of claim 78 , wherein the statin is simvastatin.
80 . The composition of claim 75 , wherein the psychotropic drug is lurasidone.
81 . The composition of any one of claim 67 to 80 , further comprising an excipient or stabilizer.
82 . The composition of claim 81 , wherein the stabilizer is lecithin.
83 . The composition of any one of claims 67 to 82 , wherein the composition is formulated for oral delivery.
84 . The composition of any one of claims 67 to 83 , wherein the composition is produced by a method comprising:
(i) producing a lipid-in-water nano-emulsion comprising the lipid droplets, the active substance, and the inulin, wherein the inulin is dissolved in the aqueous phase of the nano-emulsion; and
(ii) spray-drying the nano-emulsion.
85 . The composition of claim 84 , wherein the nano-emulsion is produced by homogenizing a mixture comprising the lipid droplets and the active substance, and adding the inulin in aqueous form to the mixture.
86 . The composition of any one of claims 67 to 85 , wherein the microparticles have an average diameter of <15 μm.
87 . A method for treating or preventing a disease or disorder in a subject, the method comprising administering the composition of any one of claims 67 to 86 to the subject.
88 . A method for treating or preventing a microbial infection in a subject, the method comprising administering the composition of any one of claims 73 to 86 to the subject, wherein the pharmaceutical agent is an antimicrobial agent.
89 . The method of claim 88 , wherein the microbial infection is a bacterial infection.
90 . The method of claim 89 , wherein the bacterial infection is due to Staphylococcus aureus.
91 . The method of claim 89 or claim 90 , wherein the bacterial infection forms part of a biofilm.
92 . A method for administering an active substance to a subject, wherein the method comprises administering to the subject a composition of any one of claims 67 to 86 .
93 . A method for producing a composition of any one of claims 67 to 86 , wherein the method comprises spray-drying a lipid-in-water nano-emulsion comprising the lipid droplets, the active substance, and the inulin.
94 . A dry composition comprising:
(i) inulin;
(ii) lipid droplets; and
(iii) lecithin,
wherein the lipid droplets are encapsulated within polymeric chains of the inulin, and wherein the inulin is not in a nano-particulate form.
95 . A method for improving the gastrointestinal health of a subject, the method comprising administering to the subject a dry composition comprising:
(i) inulin;
(ii) lipid droplets; and
(iii) lecithin,
wherein the lipid droplets are encapsulated within polymeric chains of the inulin, and wherein the inulin is not in a nano-particulate form.
96 . A method for treating or preventing a metabolic disorder or disease in a subject, the method comprising administering to the subject a dry composition comprising:
(i) inulin;
(ii) lipid droplets; and
(iii) lecithin,
wherein the lipid droplets are encapsulated within polymeric chains of the inulin, and wherein the inulin is not in a nano-particulate form.
97 . A dry composition comprising:
(i) inulin;
(ii) lipid droplets; and
(iii) a poorly water-soluble active substance,
wherein the lipid droplets are encapsulated within polymeric chains of the inulin, and wherein the inulin is not in a nano-particulate form.
98 . A method for treating or preventing a disease or disorder in a subject, the method comprising administering to the subject a dry composition comprising:
(i) inulin;
(ii) lipid droplets; and
(iii) a poorly water-soluble active substance,
wherein the lipid droplets are encapsulated within polymeric chains of the inulin, and wherein the inulin is not in a nano-particulate form.
99 . A dry composition comprising:
(i) inulin;
(ii) lipid droplets; and
(iii) an antibiotic,
wherein the lipid droplets are encapsulated within polymeric chains of the inulin, and wherein the inulin is not in a nano-particulate form.
100 . A method for treating or preventing a bacterial infection in a subject, the method comprising administering to the subject a dry composition comprising:
(i) inulin;
(ii) lipid droplets; and
(iii) an antibiotic,
wherein the lipid droplets are encapsulated within polymeric chains of the inulin, and wherein the inulin is not in a nano-particulate form.