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 . A lipid-based particle composition, comprising:
a nanoparticle comprising:
cannabidiol (CBD) 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 the nanoparticles have an average size ranging from about 75 nm to about 200 nm; and
wherein, upon storage for a period of one month, the average size of the nanoparticles changes by less than about 20%.
2 . The lipid-based particle composition of claim 1 , wherein the composition comprises liposomes and/or an oil-in-water nano-emulsion.
3 . The lipid-based particle composition of claim 1 , wherein an appreciable amount of the nanoparticle composition does not settle and/or separate from the water upon standing for a period of at least about one month at room temperature.
4 . The lipid-based particle composition of claim 1 , wherein the composition is configured such that when concentrated to dryness to afford a powder formulation of nanoparticles, the nanoparticle powder can be reconstituted to provide the nanoparticle composition.
5 . The lipid-based particle composition of claim 1 , wherein the composition has a Tmax for CBD of less than 4.5 hours.
6 . The lipid-based particle composition of claim 1 , wherein, upon storage for a period of one month, the average size of the nanoparticles changes by less than about 20%.
7 . The lipid-based particle composition of claim 1 , wherein the polydispersity of the nanoparticles in the composition is less than or equal to 0.20.
8 . The lipid-based particle composition of claim 1 , wherein upon 90 days of storage at 25° C. and 60% relative humidity, the polydispersity of the nanoparticles changes by less than or equal to 100%.
9 . The lipid-based particle composition of claim 1 , wherein upon 90 days of storage at 25° C. and 60% relative humidity, the polydispersity of the nanoparticles changes by less than or equal to 0.1.
10 . The lipid-based particle composition of claim 1 , wherein composition has a shelf life of greater than 18 months at 25° C. and 60% relative humidity.
11 . The lipid-based particle composition of claim 1 , upon 90 days of storage at 25° C. and 60% relative humidity, the D90 of the nanoparticles changes less than or equal to 10%.
12 . The lipid-based particle composition of claim 1 , wherein the composition has a concentration max (Cmax) of 80 ng/ml after an oral dose of 15 mg/kg.
13 . A lipid-based particle composition, comprising:
a particle comprising:
cannabidiol (CBD) at a weight percent in the composition ranging from 5% to 20%;
a phosphatidylcholine at a weight percent in the composition ranging from 35% to 60%;
a sterol at a weight percent in the composition ranging from 2.5% to 10%; and
a medium chain triglyceride at a weight percent in the composition ranging from 35% to 50%;
wherein the composition has a Cmax of 80 ng/ml after an oral dose of 15 mg/kg to a subject.
14 . The lipid-based particle composition of claim 13 , wherein the lipid-based particle composition is provided as a dry powder.
15 . The lipid-based particle of claim 15 , wherein the powder is configured to be reconstituted in water to provide an aqueous solution; and
wherein, upon reconstitution, nanoparticles within the aqueous solution have an average size ranging from about 75 nm to about 200 nm.
16 . The lipid-based particle composition of claim 1 , further comprising a preservative.
17 . The lipid-based particle composition of claim 16 , wherein the preservative comprises one or more of malic acid, citric acid, potassium sorbate, sodium benzoate, and Vitamin E.
18 . The lipid-based particle composition of claim 1 , wherein the sterol is cholesterol.
19 . The lipid-based particle composition of claim 1 , further comprising a flavoring agent.
20 . A method of treating a patient in need of treatment comprising administering an effective amount of the lipid-based particle composition of claim 1 to the patient.
21 .- 23 . (canceled)