Compositions for the delivery of therapeutic agents and methods of use and making thereof

Abstract

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)