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 - 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.