COMPOSITIONS FOR THE DELIVERY OF THERAPEUTIC AGENTS AND METHODS OF USE AND MAKING THEREOF
Some embodiments pertain to nanoparticle-based compositions and their use in methods for the delivery of CBD to subjects. In some embodiments, the compositions are stable for prolonged periods of time and provide enhanced bioavailability.
1 - 60 . (canceled)
61 . A lipid-based nanoparticle composition, comprising:
a hydrophobic active ingredient at a weight percent in the composition ranging from 1% to 10%;
a phosphatidylcholine at a weight percent in the composition ranging from 2.5% to 15%;
a sterol at a weight percent in the composition ranging from 0.5% to 5%; and
a medium chain triglyceride at a weight percent in the composition ranging from 2.5% to 15%; and
water at a weight percent in the composition ranging from 60% to about 80%;
wherein nanoparticles of the composition have an average size ranging from about 75 nm to about 200 nm;
wherein, when exposed to simulated gastric fluid at a pH of 1.6 and a temperature of 37° C. for a period of at least 1 hour, the average size of the nanoparticles changes less than or equal to 10%;
wherein, when exposed to simulated intestinal fluid at a pH of 6.5 and a temperature of 37° C. for a period of at least 1 hour, the average size of the nanoparticles changes less than or equal to 10%; and
wherein the nanoparticles comprise emulsion particles and liposome particles.
62 . The lipid-based nanoparticle composition of claim 61 , wherein the nanoparticles are dispersed throughout the water.
63 . The lipid-based nanoparticle composition of claim 62 , wherein the composition is configured such that an appreciable amount of the composition does not settle and/or separate from the water upon standing for a period of at least about one month at room temperature.
64 . The lipid-based nanoparticle composition of claim 61 , wherein the composition is configured such that when concentrated to dryness to afford a powder formulation of nanoparticles, the powder formulation can be reconstituted to provide the nanoparticle composition.
65 . The lipid-based nanoparticle composition of claim 61 , wherein the composition is free of surfactants and is free of emulsifiers other than phosphatidylcholine.
66 . The lipid-based nanoparticle composition of claim 61 , wherein the composition is configured such that, upon storage for a period of one month at room temperature, the average size of the nanoparticles changes by less than 20%.
67 . The lipid-based nanoparticle composition of claim 61 , wherein polydispersity of the nanoparticles in the composition is less than or equal to 0.20.
68 . The lipid-based nanoparticle composition of claim 61 , wherein the composition is configured such that upon 90 days of storage at 25° C. and 60% relative humidity, polydispersity of the nanoparticles changes by less than or equal to 100%.
69 . The lipid-based nanoparticle composition of claim 61 , wherein the composition is configured such that upon 90 days of storage at 25° C. and 60% relative humidity, polydispersity of the nanoparticles changes by less than or equal to 0.1.
70 . The lipid-based nanoparticle composition of claim 61 , wherein the composition is configured such that the composition has a shelf life of greater than 18 months at 25° C. and 60% relative humidity.
71 . The lipid-based nanoparticle composition of claim 61 , wherein the composition is configured such that upon 90 days of storage at 25° C. and 60% relative humidity, D90 of the nanoparticles changes less than or equal to 10%.
72 . The lipid-based nanoparticle composition of claim 61 , wherein the composition comprises the hydrophobic active ingredient at a weight percent in the composition ranging from 0.5% to 4%.
73 . The lipid-based nanoparticle composition of claim 61 , wherein the composition comprises the phosphatidylcholine at a weight percent in the composition ranging from 7.5% to 12.5%.
74 . The lipid-based nanoparticle composition of claim 61 , wherein the sterol is cholesterol or a phytosterol, and the composition comprises the sterol at a weight percent in the composition ranging from 0.5% to 2%.
75 . The lipid-based nanoparticle composition of claim 61 , wherein the composition comprises the medium chain triglyceride at a weight percent in the composition ranging from 7.5% to 12.5%.
76 . The lipid-based nanoparticle composition of claim 61 , wherein the composition is configured such that the composition has a concentration max (Cmax) of at least 80 ng/ml after an oral dose of 15 mg/kg.
77 . The lipid-based nanoparticle composition of claim 61 , wherein the hydrophobic active ingredient is a phytocannabinoid.
78 . A method comprising administering an amount of the composition of claim 61 to a subject.
79 . The method of claim 78 , wherein the subject is a human.
80 . The method of claim 78 , wherein the subject is a horse, dog, or cat.