Encapsulated cannabinoid formulations for oral delivery

Abstract

Preparation of cannabinoid formulations containing: Δ9-tetrahydrocannabinol (Δ9-THC), Δ8-tetrahydrocannabinol (Δ8-THC), Δ9-tetrahydrocannabinolic acid (THCa), cannabidiol (CBD), cannabidiolic acid (CBDa), cannabigerol (CBG), cannabichromene (CBC) and cannabinol (CBN), either alone or in combinations henceforth known as cannabis, have been created using an emulsification process to encapsulate cannabinoids. The aqueous-based method involves micellular encapsulation of cannabinoids, a method that has been used to increase the bioavailability of poorly permeable, lipophilic drugs. These preparations demonstrates the viability of sublingual, buccal, or oral delivery using an aqueous-based encapsulation method, including as a beverage or drink.

1 - 21 . (canceled) 
     
     
         22 . A method for preparing a cannabinoid composition having increased bioavailability, the method comprising forming a cannabinoid composition comprising:
 preparing an oil phase composition comprising:
 a cannabinoid preparation; 
 at least one surfactant; and 
 at least one co-solvent; 
   preparing a water phase composition comprising
 water; 
 at least one co-solvent; and 
 a stabilizing agent; 
   mixing the oil phase composition and the water phase composition to form micelles within a microemulsion;   wherein said cannabinoid composition yields the cannabinoid preparation capable of having increased bioavailability.   
     
     
         23 . The method of  claim 22 , wherein the at least one surfactant comprises an HLB in the range of 1 to 8 and forms a self-assembling emulsion with the at least one surfactant. 
     
     
         24 . The method of  claim 22 , wherein the at least one surfactant comprises an HLB in the range of 9-20. 
     
     
         25 . The method of  claim 22 , wherein the at least one surfactant is selected from a group consisting of: oleic acid, sunflower oil, lecithin, phosphatidylcholine, isopropyl myristate, stearic acid, medium and long chain triglycerides, Labrasol, polysorbate 20, polysorbate 80, or other ethoxylated surfactant, and sorbitan trioleate, a sorbitan surfactant, or combinations relating thereto. 
     
     
         26 . The method of  claim 22 , wherein the at least one co-solvent is selected from a group consisting of: methanol, ethanol, isopropyl alcohol, butanol, pentanol, hexanol, ethylene glycol, propylene glycol, dipropylene glycol, glycerol, glycerin, erythritol, xylitol, mannitol, sorbitol, diethylene glycol monoethyl ether (Transcutol), any derivative thereof, and combinations relating thereto. 
     
     
         27 . The method of  claim 22 , wherein the cannabinoid preparation is encapsulated by surfactants to form micelles having uni-, bi-, or multi-lamellar structures. 
     
     
         28 . The method of  claim 22 , further comprising introducing a stabilizer in the water phase composition in the range of 0.01% to 3% (w/w). 
     
     
         29 . The method of  claim 22 , further comprising introducing a thickening agent in the range of 0.01% to 10% (w/w). 
     
     
         30 . The method of  claim 22 , further comprising introducing terpenes in the range of 0.1% to 5% (w/w). 
     
     
         31 . The method of  claim 22 , further comprising sonicating the microemulsion to increase the micelles and decrease the particle size of said micelles. 
     
     
         32 . A method for preparing a cannabinoid composition having increased bioavailability, the method comprising forming a cannabinoid composition comprising:
 preparing an oil phase composition comprising:
 a cannabinoid preparation; 
 at least one surfactant; and 
 at least one co-solvent; 
   preparing a water phase composition comprising
 water; 
 at least one co-solvent; and 
 a stabilizing agent; 
   mixing the oil phase composition and the water phase composition conditions to form micelles within a microemulsion; and   introducing a second water phase composition comprising:
 water; and 
 a stabilizing agent; 
   wherein said cannabinoid composition yields the cannabinoid preparation capable of having increased bioavailability.   
     
     
         33 . The method of  claim 32 , wherein the a least one surfactant comprises an HLB in the range of 1 to 8 and forms a self-assembling emulsion with the at least one surfactant. 
     
     
         34 . The method of  claim 32 , wherein the at least one surfactant comprises an HLB in the range of 9-20. 
     
     
         35 . The method of  claim 32 , wherein the at least one surfactant is selected from a group consisting of: oleic acid, sunflower oil, lecithin, phosphatidylcholine, isopropyl myristate, stearic acid, medium and long chain triglycerides (including Labrasol), polysorbate 20, polysorbate 80, or other ethoxylated surfactant, and sorbitan trioleate, other sorbitan surfactant, or combinations thereof. 
     
     
         36 . The method of  claim 32 , wherein the at least one co-solvent is selected from a group consisting of: methanol, ethanol, isopropyl alcohol, butanol, pentanol, hexanol, ethylene glycol, propylene glycol, dipropylene glycol, glycerol, glycerin, erythritol, xylitol, mannitol, sorbitol, diethylene glycol monoethyl ether (Transcutol), any derivative thereof, and combinations relating thereto. 
     
     
         37 . The method of  claim 32 , wherein the cannabinoid preparation is encapsulated by surfactants to form micelles having uni-, bi-, or multi-lamellar structures. 
     
     
         38 . The method of  claim 32 , further comprising introducing a stabilizer in the water phase composition in the range of 0.01% to 3% (w/w). 
     
     
         39 . The method of  claim 38 , wherein the stabilizer may be a preservative or stabilizer for emulsions. 
     
     
         40 . The method of  claim 32 , further comprising introducing a thickening agent in the range of 0.01% to 10% (w/w). 
     
     
         41 . The method of  claim 32 , further comprising introducing terpenes in the range of 0.1% to 5% (w/w). 
     
     
         42 . The method of  claim 32 , further comprising sonicating the microemulsion to increase the micelles and decrease the particle size of said micelles dissolving into oil phase. 
     
     
         43 . A method for treating a subject, comprising:
 orally administering a cannabinoid composition into the subject at least once per day in a dose amount effective to treat the subject's symptoms;   wherein the oral cannabinoid composition comprises:
 an oil phase composition comprising:
 a cannabinoid preparation; 
 at least one surfactant; and 
 at least one co-solvent; 
 
 a water phase composition comprising
 water; 
 at least one co-solvent; and 
 a stabilizing agent; 
 
 wherein the oil phase composition and the water phase composition are mixed to form micelles within a microemulsion; 
   wherein said cannabinoid composition yields the cannabinoid preparation capable of having increased bioavailability when orally administered.   
     
     
         44 . The method of  claim 43 , further comprising sublingual or buccal administration. 
     
     
         45 . The method of  claim 43 , further comprising sonicating the microemulsion to increase the micelles and decrease the particle size of said micelles. 
     
     
         46 . The method of  claim 43 , wherein the cannabinoid composition is further incorporated into a beverage or drink.